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Tytuł :
Emerging Tubulin Inhibitors: A New Hope for Fungicides.
Autorzy :
Wang C; Cancer Institute, The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, Shandong 266071, People's Republic of China.
Zhang Y; The Affiliated Cardiovascular Hospital of Qingdao University, Qingdao University, Qingdao, Shandong 266071, People's Republic of China.
Xing D; Cancer Institute, The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, Shandong 266071, People's Republic of China.; School of Life Sciences, Tsinghua University, Beijing 100084, People's Republic of China.
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Źródło :
Journal of agricultural and food chemistry [J Agric Food Chem] 2021 Sep 29; Vol. 69 (38), pp. 11151-11153. Date of Electronic Publication: 2021 Sep 17.
Typ publikacji :
Journal Article
MeSH Terms :
Fungicides, Industrial*/pharmacology
Tubulin Modulators*/pharmacology
Benzimidazoles ; Tubulin/genetics
Czasopismo naukowe
Tytuł :
Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
Autorzy :
Wang Y; Henan provincial key laboratory of children's genetics and metabolic diseases, Children's Hospital Affiliated to Zhengzhou University, Zhengzhou University, Zhengzhou, 450018, China; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
Sun M; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
Wang Y; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
Qin J; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
Zhang Y; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
Pang Y; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China.
Yao Y; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China. Electronic address: .
Yang H; School of Pharmaceutical Sciences, and Institute of Drug Discovery & Development, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, Henan, 450001, China. Electronic address: .
Duan Y; Henan provincial key laboratory of children's genetics and metabolic diseases, Children's Hospital Affiliated to Zhengzhou University, Zhengzhou University, Zhengzhou, 450018, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Dec 05; Vol. 225, pp. 113790. Date of Electronic Publication: 2021 Aug 19.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Discovery*
Angiogenesis Inhibitors/*pharmacology
Antineoplastic Agents/*pharmacology
Histone Deacetylase Inhibitors/*pharmacology
Histone Deacetylases/*metabolism
Neovascularization, Physiologic/*drug effects
Tubulin Modulators/*pharmacology
Angiogenesis Inhibitors/chemical synthesis ; Angiogenesis Inhibitors/chemistry ; Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Apoptosis/drug effects ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Histone Deacetylase Inhibitors/chemical synthesis ; Histone Deacetylase Inhibitors/chemistry ; Humans ; Membrane Potential, Mitochondrial/drug effects ; Molecular Structure ; Neoplasms, Experimental/drug therapy ; Neoplasms, Experimental/metabolism ; Neoplasms, Experimental/pathology ; Polymerization/drug effects ; Structure-Activity Relationship ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry ; Zebrafish/embryology
Czasopismo naukowe
Tytuł :
Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer.
Autorzy :
Ding L; The First Hospital of Jilin University, Changchun, China.
Wei F; The First Hospital of Jilin University, Changchun, China.
Wang N; The First Hospital of Jilin University, Changchun, China.
Sun Y; The First Hospital of Jilin University, Changchun, China.
Wang Q; The First Hospital of Jilin University, Changchun, China.
Fan X; The First Hospital of Jilin University, Changchun, China.
Qi L; The Sixth Affiliated Hospital of Guangzhou Medical University, Qingyuan People's Hospital, Qingyuan, China.
Wang S; The First Hospital of Jilin University, Changchun, China.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2021 Dec; Vol. 36 (1), pp. 1563-1572.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents/*pharmacology
Enzyme Inhibitors/*pharmacology
Histone Demethylases/*antagonists & inhibitors
Liver Neoplasms/*drug therapy
Small Molecule Libraries/*pharmacology
Sulfonamides/*pharmacology
Tubulin Modulators/*pharmacology
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Histone Demethylases/metabolism ; Humans ; Liver Neoplasms/metabolism ; Liver Neoplasms/pathology ; Molecular Structure ; Polymerization/drug effects ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry ; Structure-Activity Relationship ; Sulfonamides/chemical synthesis ; Sulfonamides/chemistry ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Discovery of facile amides-functionalized rhodanine-3-acetic acid derivatives as potential anticancer agents by disrupting microtubule dynamics.
Autorzy :
Zhou X; State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guiyang, People's Republic of China.; College of Pharmacy, Guizhou University, Guiyang, People's Republic of China.
Liu J; College of Pharmacy, Guizhou University, Guiyang, People's Republic of China.
Meng J; State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guiyang, People's Republic of China.
Fu Y; College of Pharmacy, Guizhou University, Guiyang, People's Republic of China.
Wu Z; State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guiyang, People's Republic of China.
Ouyang G; College of Pharmacy, Guizhou University, Guiyang, People's Republic of China.
Wang Z; State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guiyang, People's Republic of China.; College of Pharmacy, Guizhou University, Guiyang, People's Republic of China.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2021 Dec; Vol. 36 (1), pp. 1996-2009.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Discovery*
Acetates/*pharmacology
Amides/*pharmacology
Antineoplastic Agents/*pharmacology
Microtubules/*drug effects
Rhodanine/*pharmacology
Tubulin Modulators/*pharmacology
A549 Cells ; Acetates/chemical synthesis ; Acetates/chemistry ; Amides/chemistry ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Cycle/drug effects ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Microtubules/metabolism ; Molecular Structure ; Polymerization/drug effects ; Rhodanine/analogs & derivatives ; Rhodanine/chemistry ; Structure-Activity Relationship ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation.
Autorzy :
Hagras M; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
El Deeb MA; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
Elzahabi HSA; Department of Pharmaceutical Medicinal Chemistry & Drug Design, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
Elkaeed EB; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.; Department of Pharmaceutical Sciences, College of Pharmacy, AlMaarefa University, Ad Diriyah, Riyadh, Saudi Arabia.
Mehany ABM; Department of Zoology, Faculty of Science, Al-Azhar University, Cairo, Egypt.
Eissa IH; Department of Pharmaceutical Medicinal Chemistry & Drug Design, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2021 Dec; Vol. 36 (1), pp. 640-658.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Discovery*
Molecular Docking Simulation*
Antineoplastic Agents/*pharmacology
Quinolines/*pharmacology
Tubulin Modulators/*pharmacology
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Apoptosis/drug effects ; Binding Sites/drug effects ; Cell Cycle/drug effects ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Colchicine ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Molecular Structure ; Quinolines/chemical synthesis ; Quinolines/chemistry ; Structure-Activity Relationship ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Anticancer properties of indole derivatives as IsoCombretastatin A-4 analogues.
Autorzy :
Pecnard S; Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France.
Hamze A; Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France. Electronic address: .
Bignon J; Institut de Chimie des Substances Naturelles, UPR 2301, CNRS Avenue de La Terrasse, F-91198, Gif sur Yvette, France.
Prost B; Service D'Analyse des Médicaments et Métabolites, IPSIT, Univ. Paris-Sud, UMS 3679 CNRS, US 31 INSERM, Université Paris-Saclay, 92290, Châtenay Malabry, France.
Deroussent A; Metabolic and Systemic Aspects of Oncogenesis (METSY), UMR 9018, CNRS, Institut Gustave Roussy, Université Paris-Saclay, 94805, Villejuif, France.
Gallego-Yerga L; Laboratorio de Química Orgánica y Farmacéutica, Departamento de Ciencias Farmacéuticas, Facultad de Farmacia, Universidad de Salamanca, Salamanca, Spain.
Peláez R; Laboratorio de Química Orgánica y Farmacéutica, Departamento de Ciencias Farmacéuticas, Facultad de Farmacia, Universidad de Salamanca, Salamanca, Spain.
Paik JY; Department of Pharmacy, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 08626, South Korea.
Diederich M; Department of Pharmacy, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 08626, South Korea.
Alami M; Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France. Electronic address: .
Provot O; Université Paris-Saclay, CNRS, BioCIS, 92290, Châtenay-Malabry, France. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113656. Date of Electronic Publication: 2021 Jun 18.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents/*pharmacology
Indoles/*chemistry
Stilbenes/*chemistry
Tubulin Modulators/*chemistry
Animals ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/metabolism ; Binding Sites ; Cell Cycle Checkpoints/drug effects ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Resistance, Neoplasm/drug effects ; Drug Screening Assays, Antitumor ; Drug Stability ; Humans ; Indoles/metabolism ; Indoles/pharmacology ; Microsomes, Liver/metabolism ; Molecular Docking Simulation ; Rats ; Stilbenes/metabolism ; Stilbenes/pharmacology ; Structure-Activity Relationship ; Tubulin/chemistry ; Tubulin/metabolism ; Tubulin Modulators/metabolism ; Tubulin Modulators/pharmacology
Czasopismo naukowe
Tytuł :
Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors.
Autorzy :
Wu CJ; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, PR China.
Wu JQ; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, PR China.
Hu Y; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, PR China.
Pu S; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, PR China.
Lin Y; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, PR China.
Zeng Z; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, PR China.
Hu J; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, PR China. Electronic address: .
Chen WH; School of Biotechnology and Health Sciences, Wuyi University, Jiangmen, 529020, PR China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113629. Date of Electronic Publication: 2021 Jun 17.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents/*pharmacology
Indoles/*pharmacology
Pyridines/*pharmacology
Triazoles/*pharmacology
Tubulin Modulators/*pharmacology
Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/metabolism ; Apoptosis/drug effects ; Cattle ; Cell Line, Tumor ; Cell Movement/drug effects ; Cell Proliferation/drug effects ; Drug Design ; G2 Phase Cell Cycle Checkpoints/drug effects ; Humans ; Indoles/chemical synthesis ; Indoles/metabolism ; Molecular Docking Simulation ; Molecular Structure ; Protein Binding ; Pyridines/chemical synthesis ; Pyridines/metabolism ; Rats ; Structure-Activity Relationship ; Triazoles/chemical synthesis ; Triazoles/metabolism ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/metabolism
Czasopismo naukowe
Tytuł :
Microtubule associated proteins as targets for anticancer drug development.
Autorzy :
Khwaja S; CSIR-Central Institute of Medicinal and Aromatics Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow 226015, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India.
Kumar K; CSIR-Central Institute of Medicinal and Aromatics Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow 226015, India.
Das R; CSIR-Central Institute of Medicinal and Aromatics Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow 226015, India.
Negi AS; CSIR-Central Institute of Medicinal and Aromatics Plants (CSIR-CIMAP) P.O. CIMAP, Lucknow 226015, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address: .
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Źródło :
Bioorganic chemistry [Bioorg Chem] 2021 Nov; Vol. 116, pp. 105320. Date of Electronic Publication: 2021 Sep 01.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't; Review
MeSH Terms :
Drug Development*
Antineoplastic Agents/*pharmacology
Histone Deacetylase Inhibitors/*pharmacology
Microtubule-Associated Proteins/*antagonists & inhibitors
Tubulin Modulators/*pharmacology
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Histone Deacetylase Inhibitors/chemical synthesis ; Histone Deacetylase Inhibitors/chemistry ; Histone Deacetylases/metabolism ; Humans ; Microtubule-Associated Proteins/metabolism ; Molecular Structure ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Lattice defects induced by microtubule-stabilizing agents exert a long-range effect on microtubule growth by promoting catastrophes.
Autorzy :
Rai A; Cell Biology, Neurobiology and Biophysics, Department of Biology, Faculty of Science, Utrecht University 3584 CH Utrecht, the Netherlands.
Liu T; Institute of Structural and Molecular Biology, Birkbeck, University of London, WC1E 7HX London, United Kingdom.
Katrukha EA; Cell Biology, Neurobiology and Biophysics, Department of Biology, Faculty of Science, Utrecht University 3584 CH Utrecht, the Netherlands.
Estévez-Gallego J; Structural and Chemical Biology, Centro de Investigaciones Biológicas Margarita Salas, Consejo Superior de Investigaciones Científicas 28040 Madrid, Spain.
Manka SW; Institute of Structural and Molecular Biology, Birkbeck, University of London, WC1E 7HX London, United Kingdom.
Paterson I; Yusuf Hamied Department of Chemistry, University of Cambridge, Cambridge CB2 1EW, United Kingdom.
Díaz JF; Structural and Chemical Biology, Centro de Investigaciones Biológicas Margarita Salas, Consejo Superior de Investigaciones Científicas 28040 Madrid, Spain.
Kapitein LC; Cell Biology, Neurobiology and Biophysics, Department of Biology, Faculty of Science, Utrecht University 3584 CH Utrecht, the Netherlands.
Moores CA; Institute of Structural and Molecular Biology, Birkbeck, University of London, WC1E 7HX London, United Kingdom.
Akhmanova A; Cell Biology, Neurobiology and Biophysics, Department of Biology, Faculty of Science, Utrecht University 3584 CH Utrecht, the Netherlands; .
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Źródło :
Proceedings of the National Academy of Sciences of the United States of America [Proc Natl Acad Sci U S A] 2021 Dec 21; Vol. 118 (51).
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Microtubules/*metabolism
Tubulin Modulators/*metabolism
Biological Phenomena ; Microtubule-Associated Proteins/chemistry ; Microtubule-Associated Proteins/metabolism ; Microtubules/chemistry ; Microtubules/ultrastructure ; Paclitaxel/metabolism ; Polymerization ; Protein Binding ; Tubulin/chemistry ; Tubulin/metabolism ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Design, synthesis and biological evaluation of 1-Aryl-5-(4-arylpiperazine-1-carbonyl)-1 H -tetrazols as novel microtubule destabilizers.
Autorzy :
Wang C; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, China.
Li Y; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, China.
Liu Z; Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang, China.
Wang Z; Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, China.
Liu Z; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, China.
Man S; Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang, China.
Zhang Y; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, China.
Bao K; Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, China.
Wu Y; Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang, China.
Guan Q; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, China.
Zuo D; Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang, China.
Zhang W; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, China.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2021 Dec; Vol. 36 (1), pp. 549-560.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Antineoplastic Agents/*pharmacology
Microtubules/*drug effects
Tetrazoles/*pharmacology
Tubulin Modulators/*pharmacology
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Cycle/drug effects ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Microtubules/metabolism ; Microwaves ; Models, Molecular ; Molecular Structure ; Polymerization/drug effects ; Structure-Activity Relationship ; Tetrazoles/chemical synthesis ; Tetrazoles/chemistry ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry ; Tumor Cells, Cultured
Czasopismo naukowe
Tytuł :
A new class of cytotoxic agents targets tubulin and disrupts microtubule dynamics.
Autorzy :
Al-Hamashi AA; Department of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Koranne R; Department of Biological Sciences, College of Natural Sciences and Mathematics, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Dlamini S; Department of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Alqahtani A; Department of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Karaj E; Department of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Rashid MS; Department of Biological Sciences, College of Natural Sciences and Mathematics, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA.
Knoff JR; Department of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI 48202, USA.
Dunworth M; The Sidney Kimmel Comprehensive Cancer Center, The Johns Hopkins University School of Medicine, Bunting/Blaustein Cancer Research Building 1 1650 Orleans Street - Room 551, Baltimore, MD 21231, USA.
Pflum MKH; Department of Chemistry, Wayne State University, 5101 Cass Avenue, Detroit, MI 48202, USA.
Casero RA Jr; The Sidney Kimmel Comprehensive Cancer Center, The Johns Hopkins University School of Medicine, Bunting/Blaustein Cancer Research Building 1 1650 Orleans Street - Room 551, Baltimore, MD 21231, USA.
Perera L; Laboratory of Genome Integrity and Structural Biology, National Institute of Environmental Health Sciences, National Institutes of Health, Department of Health and Human Services, Research Triangle Park, NC 27709, USA.
Taylor WR; Department of Biological Sciences, College of Natural Sciences and Mathematics, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA. Electronic address: .
Tillekeratne LMV; Department of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 2801, W. Bancroft Street, Toledo, OH-43606, USA. Electronic address: .
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Źródło :
Bioorganic chemistry [Bioorg Chem] 2021 Nov; Vol. 116, pp. 105297. Date of Electronic Publication: 2021 Aug 30.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, N.I.H., Intramural
MeSH Terms :
Antineoplastic Agents/*pharmacology
Cytotoxins/*pharmacology
Ethanol/*pharmacology
Imidazoles/*pharmacology
Microtubules/*drug effects
Tubulin Modulators/*pharmacology
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Cytotoxins/chemical synthesis ; Cytotoxins/chemistry ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Ethanol/analogs & derivatives ; Ethanol/chemistry ; HCT116 Cells ; Humans ; Imidazoles/chemical synthesis ; Imidazoles/chemistry ; Microtubules/metabolism ; Molecular Structure ; Polymerization/drug effects ; Structure-Activity Relationship ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry ; Tumor Cells, Cultured
Czasopismo naukowe
Tytuł :
Discovery of pyrrole derivatives for the treatment of glioblastoma and chronic myeloid leukemia.
Autorzy :
Puxeddu M; Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.
Shen H; Department of Urology, Capital Medical University Beijing Friendship Hospital, Beijing, 100050, China.
Bai R; Molecular Pharmacology Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, Frederick National Laboratory for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD, 21702, United States.
Coluccia A; Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.
Bufano M; Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.
Nalli M; Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.
Sebastiani J; Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.
Brancaccio D; Department of Pharmacy, University of Naples'Federico II', Via Domenico Montesano 49, 80131, Naples, Italy.
Da Pozzo E; Department of Pharmacy, University of Pisa, Via Bonanno Pisano 6, I-56126, Pisa, Italy.
Tremolanti C; Department of Pharmacy, University of Pisa, Via Bonanno Pisano 6, I-56126, Pisa, Italy.
Martini C; Department of Pharmacy, University of Pisa, Via Bonanno Pisano 6, I-56126, Pisa, Italy.
Orlando V; Department of Biology and Biotechnologies 'Charles Darwin', Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.
Biagioni S; Department of Biology and Biotechnologies 'Charles Darwin', Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy.
Sinicropi MS; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, I-87036, Rende, Cosenza, Italy.
Ceramella J; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, I-87036, Rende, Cosenza, Italy.
Iacopetta D; Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, I-87036, Rende, Cosenza, Italy.
Coluccia AML; Department of Biological and Environmental Sciences and Technologies, University of Salento, I-73100, Lecce, Italy.
Hamel E; Molecular Pharmacology Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, Frederick National Laboratory for Cancer Research, National Cancer Institute, National Institutes of Health, Frederick, MD, 21702, United States.
Liu T; Department of Biological and Environmental Sciences and Technologies, University of Salento, I-73100, Lecce, Italy; Shanghai Geriatric Institute of Chinese Medicine, Shanghai University of Traditional Chinese Medicine, 365 South Xiangyang Road, Shanghai, 200031, China. Electronic address: .
Silvestri R; Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy. Electronic address: .
La Regina G; Laboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185, Roma, Italy. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Oct 05; Vol. 221, pp. 113532. Date of Electronic Publication: 2021 May 05.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Discovery*
Antineoplastic Agents/*pharmacology
Glioblastoma/*drug therapy
Heterocyclic Compounds/*pharmacology
Leukemia, Myelogenous, Chronic, BCR-ABL Positive/*drug therapy
Methane/*pharmacology
Tubulin Modulators/*pharmacology
Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Female ; Glioblastoma/metabolism ; Glioblastoma/pathology ; Heterocyclic Compounds/chemical synthesis ; Heterocyclic Compounds/chemistry ; Humans ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive/metabolism ; Leukemia, Myelogenous, Chronic, BCR-ABL Positive/pathology ; Methane/analogs & derivatives ; Methane/chemistry ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Molecular Structure ; Neoplasms, Experimental/drug therapy ; Neoplasms, Experimental/metabolism ; Neoplasms, Experimental/pathology ; Polymerization/drug effects ; Structure-Activity Relationship ; Tubulin/metabolism ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry ; Tumor Cells, Cultured
Czasopismo naukowe
Tytuł :
1H-benzimidazole-2-yl hydrazones as tubulin-targeting agents: Synthesis, structural characterization, anthelmintic activity and antiproliferative activity against MCF-7 breast carcinoma cells and molecular docking studies.
Autorzy :
Anichina K; University of Chemical Technology and Metallurgy, 8 Kliment Ohridski Blvd., 1756, Sofia, Bulgaria.
Argirova M; Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., build. 9, 1113 Sofia, Bulgaria.
Tzoneva R; Institute of Biophysics and Biomedical Engineering, Bulgarian Academy of Sciences, 1113, Sofia, Bulgaria.
Uzunova V; Institute of Biophysics and Biomedical Engineering, Bulgarian Academy of Sciences, 1113, Sofia, Bulgaria.
Mavrova A; University of Chemical Technology and Metallurgy, 8 Kliment Ohridski Blvd., 1756, Sofia, Bulgaria.
Vuchev D; Departmant of Infectious Diseases, Parasitology and Tropical Medicine, Medical University, Plovdiv, Bulgaria.
Popova-Daskalova G; Departmant of Infectious Diseases, Parasitology and Tropical Medicine, Medical University, Plovdiv, Bulgaria.
Fratev F; Micar Innovation (Micar 21) Ltd., 34B Persenk Str., 1407, Sofia, Bulgaria; Department of Pharmaceutical Sciences, School of Pharmacy, The University of Texas at El Paso, 1101 N Campbell St, El Paso, TX, 79968, USA.
Guncheva M; Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., build. 9, 1113 Sofia, Bulgaria.
Yancheva D; Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, Acad. G. Bonchev Str., build. 9, 1113 Sofia, Bulgaria. Electronic address: .
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Źródło :
Chemico-biological interactions [Chem Biol Interact] 2021 Aug 25; Vol. 345, pp. 109540. Date of Electronic Publication: 2021 Jun 15.
Typ publikacji :
Journal Article
MeSH Terms :
Molecular Docking Simulation*
Benzimidazoles/*chemistry
Hydrazones/*chemistry
Hydrazones/*pharmacology
Tubulin/*metabolism
Anthelmintics/chemical synthesis ; Anthelmintics/chemistry ; Anthelmintics/metabolism ; Anthelmintics/pharmacology ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Cell Proliferation/drug effects ; Chemistry Techniques, Synthetic ; Drug Design ; Drug Screening Assays, Antitumor ; Humans ; Hydrazones/chemical synthesis ; Hydrazones/metabolism ; MCF-7 Cells ; Protein Conformation ; Structure-Activity Relationship ; Tubulin/chemistry ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry ; Tubulin Modulators/metabolism ; Tubulin Modulators/pharmacology
Czasopismo naukowe
Tytuł :
C118P, a novel microtubule inhibitor with anti-angiogenic and vascular disrupting activities, exerts anti-tumor effects against hepatocellular carcinoma.
Autorzy :
Yang M; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009 China.
Su Y; Zhuhai Interventional Medical Center, Zhuhai Precision Medical Center, Zhuhai People's Hospital (Zhuhai Hospital affiliated with Jinan University), Zhuhai 519000 China.
Wang Z; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009 China.
Du D; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009 China.
Wei S; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009 China.
Liao Z; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009 China.
Zhang Q; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009 China.
Zhao L; Nanjing Sanhome Pharmaceutical Co. Ltd., Nanjing 211135 China.
Zhang X; Nanjing Sanhome Pharmaceutical Co. Ltd., Nanjing 211135 China.
Han L; Nanjing Sanhome Pharmaceutical Co. Ltd., Nanjing 211135 China.
Jiang J; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009 China.
Zhan M; Zhuhai Interventional Medical Center, Zhuhai Precision Medical Center, Zhuhai People's Hospital (Zhuhai Hospital affiliated with Jinan University), Zhuhai 519000 China.
Sun L; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009 China. Electronic address: .
Yuan S; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009 China. Electronic address: .
Zhou Z; Department of Pharmacy, Zhuhai People's Hospital (Zhuhai Hospital affiliated with Jinan University), Zhuhai 519000 China. Electronic address: .
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Źródło :
Biochemical pharmacology [Biochem Pharmacol] 2021 Aug; Vol. 190, pp. 114641. Date of Electronic Publication: 2021 May 30.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Carcinoma, Hepatocellular/*drug therapy
Liver Neoplasms/*drug therapy
Microtubules/*drug effects
Neovascularization, Pathologic/*prevention & control
Tubulin Modulators/*pharmacology
Animals ; Antineoplastic Agents ; Apoptosis ; Blood Vessels ; Cell Cycle Checkpoints/drug effects ; Cell Line, Tumor ; Human Umbilical Vein Endothelial Cells ; Humans ; Male ; Mice ; Neoplasms, Experimental/drug therapy ; Protein Conformation ; Tubulin/chemistry ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Design, synthesis and biological evaluation of novel thiazole-naphthalene derivatives as potential anticancer agents and tubulin polymerisation inhibitors.
Autorzy :
Wang G; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.
Liu W; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.; School of Pharmacy, Guizhou Medical University, Guiyang, China.
Fan M; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.; School of Pharmacy, Guizhou Medical University, Guiyang, China.
He M; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China.; School of Pharmacy, Guizhou Medical University, Guiyang, China.
Li Y; Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, China.
Peng Z; College of Food Science and Technology, Shanghai Ocean University, Shanghai, China.
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Źródło :
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2021 Dec; Vol. 36 (1), pp. 1694-1702.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Antineoplastic Agents/*pharmacology
Naphthalenes/*pharmacology
Thiazoles/*pharmacology
Tubulin/*metabolism
Tubulin Modulators/*pharmacology
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Apoptosis/drug effects ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Humans ; Molecular Docking Simulation ; Molecular Structure ; Naphthalenes/chemical synthesis ; Naphthalenes/chemistry ; Polymerization/drug effects ; Structure-Activity Relationship ; Thiazoles/chemical synthesis ; Thiazoles/chemistry ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Identification and optimization of biphenyl derivatives as novel tubulin inhibitors targeting colchicine-binding site overcoming multidrug resistance.
Autorzy :
Cheng B; Research Center for Molecular Recognition and Synthesis, Department of Chemistry, Fudan University, 220 Handan Lu, Shanghai, 200433, PR China.
Zhu G; Research Center for Molecular Recognition and Synthesis, Department of Chemistry, Fudan University, 220 Handan Lu, Shanghai, 200433, PR China.
Meng L; Research Center for Molecular Recognition and Synthesis, Department of Chemistry, Fudan University, 220 Handan Lu, Shanghai, 200433, PR China.
Wu G; Research Center for Molecular Recognition and Synthesis, Department of Chemistry, Fudan University, 220 Handan Lu, Shanghai, 200433, PR China.
Chen Q; Research Center for Molecular Recognition and Synthesis, Department of Chemistry, Fudan University, 220 Handan Lu, Shanghai, 200433, PR China. Electronic address: .
Ma S; Research Center for Molecular Recognition and Synthesis, Department of Chemistry, Fudan University, 220 Handan Lu, Shanghai, 200433, PR China; State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai, 200032, PR China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2022 Jan 15; Vol. 228, pp. 113930. Date of Electronic Publication: 2021 Oct 20.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents/*pharmacology
Biphenyl Compounds/*pharmacology
Colchicine/*pharmacology
Drug Resistance, Multiple/*drug effects
Tubulin/*metabolism
Tubulin Modulators/*pharmacology
Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Binding Sites/drug effects ; Biphenyl Compounds/chemical synthesis ; Biphenyl Compounds/chemistry ; Cell Proliferation/drug effects ; Colchicine/chemistry ; Dose-Response Relationship, Drug ; Drug Resistance, Neoplasm/drug effects ; Drug Screening Assays, Antitumor ; Female ; Humans ; Mammary Neoplasms, Experimental/drug therapy ; Mammary Neoplasms, Experimental/metabolism ; Mammary Neoplasms, Experimental/pathology ; Mice ; Mice, Inbred BALB C ; Microtubules/drug effects ; Microtubules/metabolism ; Molecular Structure ; Polymerization/drug effects ; Structure-Activity Relationship ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry ; Tumor Cells, Cultured
Czasopismo naukowe
Tytuł :
Discovery of novel tubulin inhibitors targeting the colchicine binding site via virtual screening, structural optimization and antitumor evaluation.
Autorzy :
Liu W; Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi Province, China; Faculty of Pharmacy, School of Food and Biological Engineering, Shaanxi University of Science and Technology, Xi'an, Shaanxi Province, China.
Jia H; Faculty of Pharmacy, School of Food and Biological Engineering, Shaanxi University of Science and Technology, Xi'an, Shaanxi Province, China.
Guan M; Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi Province, China.
Cui M; Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi Province, China.
Lan Z; Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi Province, China.
He Y; Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi Province, China.
Guo Z; Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi Province, China.
Jiang R; Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi Province, China.
Dong G; Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai, China.
Wang S; Department of Medicinal Chemistry and Pharmaceutical Analysis, School of Pharmacy, Fourth Military Medical University, Xi'an, Shaanxi Province, China. Electronic address: .
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Źródło :
Bioorganic chemistry [Bioorg Chem] 2022 Jan; Vol. 118, pp. 105486. Date of Electronic Publication: 2021 Nov 14.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Drug Discovery*
Antineoplastic Agents/*pharmacology
Tubulin/*metabolism
Tubulin Modulators/*pharmacology
Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Evaluation, Preclinical ; Drug Screening Assays, Antitumor ; Humans ; Models, Molecular ; Molecular Structure ; Polymerization/drug effects ; Structure-Activity Relationship ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Synthesis of N-acyl Derivatives of Aminocombretastatin A-4 and Study of their Interaction with Tubulin and Downregulation of c-Myc.
Autorzy :
Agut R; Dpto. de Quimica Inorganica y Organica, Universidad Jaume I, E-12071 Castellon, Spain.
Falomir E; Dpto. de Quimica Inorganica y Organica, Universidad Jaume I, E-12071 Castellon, Spain.
Murga J; Dpto. de Quimica Inorganica y Organica, Universidad Jaume I, E-12071 Castellon, Spain.
Martín-Beltrán C; Dpto. de Quimica Inorganica y Organica, Universidad Jaume I, E-12071 Castellon, Spain.
Gil-Edo R; Dpto. de Quimica Inorganica y Organica, Universidad Jaume I, E-12071 Castellon, Spain.
Pla A; Dpto. de Quimica Inorganica y Organica, Universidad Jaume I, E-12071 Castellon, Spain.
Carda M; Dpto. de Quimica Inorganica y Organica, Universidad Jaume I, E-12071 Castellon, Spain.
Díaz JF; CIB, Consejo Superior de Investigaciones Científicas, E-28040 Madrid, Spain.
Josa-Prado F; CIB, Consejo Superior de Investigaciones Científicas, E-28040 Madrid, Spain.
Marco JA; Dept. de Quimica Organica, Universidad de Valencia, 46100 Burjassot, Valencia, Spain.
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Źródło :
Medicinal chemistry (Shariqah (United Arab Emirates)) [Med Chem] 2021; Vol. 17 (10), pp. 1129-1139.
Typ publikacji :
Journal Article
MeSH Terms :
Antineoplastic Agents*/pharmacology
Tubulin*/metabolism
Cell Line, Tumor ; Cell Proliferation ; Down-Regulation ; Drug Screening Assays, Antitumor ; Humans ; Molecular Docking Simulation ; Structure-Activity Relationship ; Tubulin Modulators/pharmacology
Czasopismo naukowe
Tytuł :
Design, synthesis and bioevaluation of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazoles as tubulin polymerization inhibitors.
Autorzy :
Liu R; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, China.
Huang M; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, China.
Zhang S; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, China.
Li L; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, China.
Li M; School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, China.
Sun J; Clinical Pharmacology Laboratory, Henan Province People's Hospital, Zhengzhou University People's Hospital, 7 Weiwu Road, Jinshui District, Zhengzhou, 450003, China.
Wu L; Department of Geratology, The First Affiliated Hospital, Chinese Medical University, Shenyang, 110001, China. Electronic address: .
Guan Q; School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, China. Electronic address: .
Zhang W; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Dec 15; Vol. 226, pp. 113826. Date of Electronic Publication: 2021 Sep 11.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Design*
Antineoplastic Agents/*pharmacology
Imidazoles/*pharmacology
Tubulin/*metabolism
Tubulin Modulators/*pharmacology
Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Apoptosis/drug effects ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Female ; Humans ; Imidazoles/chemical synthesis ; Imidazoles/chemistry ; Mammary Neoplasms, Experimental/drug therapy ; Mammary Neoplasms, Experimental/pathology ; Mice ; Mice, Inbred BALB C ; Molecular Docking Simulation ; Molecular Structure ; Polymerization/drug effects ; Structure-Activity Relationship ; Tubulin Modulators/chemical synthesis ; Tubulin Modulators/chemistry
Czasopismo naukowe
Tytuł :
Comprehensive Analysis of Binding Sites in Tubulin.
Autorzy :
Mühlethaler T; Laboratory of Biomolecular Research, Department of Biology and Chemistry, Paul Scherrer Institut, 5232, Villigen PSI, Switzerland.
Gioia D; Computational & Chemical Biology, Istituto Italiano di Tecnologia, via Morego, 30, 16163, Genova, Italy.
Prota AE; Laboratory of Biomolecular Research, Department of Biology and Chemistry, Paul Scherrer Institut, 5232, Villigen PSI, Switzerland.
Sharpe ME; Swiss Light Source, Paul Scherrer Institut, 5232, Villigen PSI, Switzerland.
Cavalli A; Computational & Chemical Biology, Istituto Italiano di Tecnologia, via Morego, 30, 16163, Genova, Italy.; Department of Pharmacy and Biotechnology, Alma Mater Studiorum, University of Bologna, via Belmeloro 6, 40126, Bologna, Italy.
Steinmetz MO; Laboratory of Biomolecular Research, Department of Biology and Chemistry, Paul Scherrer Institut, 5232, Villigen PSI, Switzerland.; University of Basel, Biozentrum, 4056, Basel, Switzerland.
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Źródło :
Angewandte Chemie (International ed. in English) [Angew Chem Int Ed Engl] 2021 Jun 07; Vol. 60 (24), pp. 13331-13342. Date of Electronic Publication: 2021 May 05.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Ligands*
Tubulin/*metabolism
Allosteric Regulation ; Binding Sites ; Crystallography, X-Ray ; Molecular Dynamics Simulation ; Protein Binding ; Tubulin/chemistry ; Tubulin Modulators/chemistry ; Tubulin Modulators/metabolism
Czasopismo naukowe

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