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Tytuł :
Assessing the pharmacokinetics of acalabrutinib in the treatment of chronic lymphocytic leukemia.
Autorzy :
Miao Y; Department of Hematology, The First Affiliated Hospital of Nanjing Medical University, Jiangsu Province Hospital, Nanjing, China.; Key Laboratory of Hematology of Nanjing Medical University, Nanjing, China.; Pukou CLL Center, Nanjing, China.
Xu W; Department of Hematology, The First Affiliated Hospital of Nanjing Medical University, Jiangsu Province Hospital, Nanjing, China.; Key Laboratory of Hematology of Nanjing Medical University, Nanjing, China.; Pukou CLL Center, Nanjing, China.
Li J; Department of Hematology, The First Affiliated Hospital of Nanjing Medical University, Jiangsu Province Hospital, Nanjing, China.; Key Laboratory of Hematology of Nanjing Medical University, Nanjing, China.; Pukou CLL Center, Nanjing, China.
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Źródło :
Expert opinion on drug metabolism & toxicology [Expert Opin Drug Metab Toxicol] 2021 Sep; Vol. 17 (9), pp. 1023-1030. Date of Electronic Publication: 2021 Jul 28.
Typ publikacji :
Comparative Study; Journal Article; Review
MeSH Terms :
Antineoplastic Agents/*administration & dosage
Benzamides/*administration & dosage
Leukemia, Lymphocytic, Chronic, B-Cell/*drug therapy
Pyrazines/*administration & dosage
Adenine/administration & dosage ; Adenine/adverse effects ; Adenine/analogs & derivatives ; Agammaglobulinaemia Tyrosine Kinase/antagonists & inhibitors ; Animals ; Antineoplastic Agents/adverse effects ; Antineoplastic Agents/pharmacokinetics ; Benzamides/adverse effects ; Benzamides/pharmacokinetics ; Humans ; Leukemia, Lymphocytic, Chronic, B-Cell/pathology ; Piperidines/administration & dosage ; Piperidines/adverse effects ; Protein Kinase Inhibitors/administration & dosage ; Protein Kinase Inhibitors/adverse effects ; Protein Kinase Inhibitors/pharmacokinetics ; Pyrazines/adverse effects ; Pyrazines/pharmacokinetics
Czasopismo naukowe
Tytuł :
Residues and dietary intake risk assessments of clomazone, fomesafen, haloxyfop-methyl and its metabolite haloxyfop in spring soybean field ecosystem.
Autorzy :
Liang Y; College of Chemistry and Biological Engineering, University of Science and Technology Beijing, Beijing 100083, PR China.
Wei L; College of Chemistry and Biological Engineering, University of Science and Technology Beijing, Beijing 100083, PR China.
Hu J; College of Chemistry and Biological Engineering, University of Science and Technology Beijing, Beijing 100083, PR China. Electronic address: .
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Źródło :
Food chemistry [Food Chem] 2021 Oct 30; Vol. 360, pp. 129921. Date of Electronic Publication: 2021 Apr 22.
Typ publikacji :
Journal Article
MeSH Terms :
Ecosystem*
Benzamides/*analysis
Herbicides/*analysis
Isoxazoles/*analysis
Oxazolidinones/*analysis
Pesticide Residues/*analysis
Pyridines/*analysis
Soybeans/*chemistry
Benzamides/toxicity ; Chromatography, High Pressure Liquid/methods ; Humans ; Isoxazoles/toxicity ; Oxazolidinones/toxicity ; Pyridines/toxicity ; Risk Assessment ; Seasons ; Tandem Mass Spectrometry/methods
Czasopismo naukowe
Tytuł :
Phase I clinical trial of HC-1119: A deuterated form of enzalutamide.
Autorzy :
Li X; Institute of Clinical Pharmacology, GCP center, West China Hospital, Sichuan University, Chengdu, China.; State Key Laboratory of Biotherapy, Sichuan University, Chengdu, China.
Cheng K; Department of Abdominal Oncology, West China Hospital, Sichuan University, Chengdu, China.
Li X; Hinova Pharmaceuticals Inc., Chengdu, China.
Zhou Y; Department of Biotherapy, Cancer Center of West China Hospital, Sichuan University, Chengdu, China.
Liu J; Department of Biotherapy, Cancer Center of West China Hospital, Sichuan University, Chengdu, China.
Zeng H; Department of Urology, Institute of Urology, West China Hospital, Sichuan University, Chengdu, China.
Chen Y; Hinova Pharmaceuticals Inc., Chengdu, China.
Liu X; Haisco Pharmaceuticals Inc., Shanghai, China.
Zhang Y; Haisco Pharmaceuticals Inc., Shanghai, China.
Wang Y; State Key Laboratory of Biotherapy, Sichuan University, Chengdu, China.; Institute of Clinical Pharmacology, GCP center, Department of Thoracic, Chengdu, China.
Bi F; Department of Abdominal Oncology, West China Hospital, Sichuan University, Chengdu, China.
Zheng L; Institute of Clinical Pharmacology, GCP center, West China Hospital, Sichuan University, Chengdu, China.
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Źródło :
International journal of cancer [Int J Cancer] 2021 Oct 01; Vol. 149 (7), pp. 1473-1482. Date of Electronic Publication: 2021 Jul 07.
Typ publikacji :
Clinical Trial, Phase I; Journal Article; Multicenter Study; Research Support, Non-U.S. Gov't
MeSH Terms :
Adenocarcinoma/*drug therapy
Antineoplastic Agents/*therapeutic use
Benzamides/*therapeutic use
Nitriles/*therapeutic use
Phenylthiohydantoin/*therapeutic use
Prostatic Neoplasms/*drug therapy
Adenocarcinoma/secondary ; Aged ; Aged, 80 and over ; Antineoplastic Agents/pharmacokinetics ; Benzamides/pharmacokinetics ; Follow-Up Studies ; Humans ; Male ; Maximum Tolerated Dose ; Middle Aged ; Nitriles/pharmacokinetics ; Phenylthiohydantoin/pharmacokinetics ; Prognosis ; Prostatic Neoplasms/pathology ; Tissue Distribution
Czasopismo naukowe
Tytuł :
Distribution of fluopyram and tebuconazole in pomegranate tissues and their risk assessment.
Autorzy :
Yogendraiah Matadha N; Pesticide Residue Laboratory, ICAR-Indian Institute of Horticultural Research, Hesaraghatta Lake Post, Bangalore 560089, India.
Mohapatra S; Pesticide Residue Laboratory, ICAR-Indian Institute of Horticultural Research, Hesaraghatta Lake Post, Bangalore 560089, India. Electronic address: .
Siddamallaiah L; Pesticide Residue Laboratory, ICAR-Indian Institute of Horticultural Research, Hesaraghatta Lake Post, Bangalore 560089, India.
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Źródło :
Food chemistry [Food Chem] 2021 Oct 01; Vol. 358, pp. 129909. Date of Electronic Publication: 2021 Apr 20.
Typ publikacji :
Journal Article
MeSH Terms :
Benzamides/*analysis
Food Contamination/*analysis
Pomegranate/*chemistry
Pyridines/*analysis
Triazoles/*analysis
Benzamides/pharmacokinetics ; Dietary Exposure/adverse effects ; Fruit/chemistry ; Fungicides, Industrial/analysis ; Humans ; Pesticide Residues/analysis ; Plant Leaves/chemistry ; Pyridines/pharmacokinetics ; Risk Assessment ; Triazoles/pharmacokinetics
Czasopismo naukowe
Tytuł :
Combined Therapy of ATRA and Imatinib Mesylate Decreases BCR-ABL and ABCB1/MDR1 Expression Through Cellular Differentiation in a Chronic Myeloid Leukemia Model.
Autorzy :
Pinto CA; Human Cytogenetics Laboratory, Biological Science Institute, Federal University of Pará, Belém, Brazil.
DE Sousa Portilho AJ; Pharmacogenetics Laboratory, Drug Research and Development Center (NPDM), Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, Brazil.
Barbosa MC; Faculty of Pharmacy, Federal University of Ceará, Fortaleza, Brazil.
DE Moraes MEA; Pharmacogenetics Laboratory, Drug Research and Development Center (NPDM), Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, Brazil.
DE Lemos JAR; Biological Science Institute, Federal University of Pará, Belém, Brazil.
Burbano RMR; Human Cytogenetics Laboratory, Biological Science Institute, Federal University of Pará, Belém, Brazil.
Moreira-Nunes CA; Pharmacogenetics Laboratory, Drug Research and Development Center (NPDM), Department of Physiology and Pharmacology, Federal University of Ceará, Fortaleza, Brazil; .
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Źródło :
In vivo (Athens, Greece) [In Vivo] 2021 Sep-Oct; Vol. 35 (5), pp. 2661-2667.
Typ publikacji :
Journal Article
MeSH Terms :
Benzamides*
Leukemia, Myelogenous, Chronic, BCR-ABL Positive*/drug therapy
Leukemia, Myelogenous, Chronic, BCR-ABL Positive*/genetics
ATP Binding Cassette Transporter, Subfamily B/genetics ; Apoptosis ; Cell Differentiation ; Drug Resistance, Neoplasm/genetics ; Fusion Proteins, bcr-abl/genetics ; Humans ; Imatinib Mesylate/pharmacology ; Piperazines ; Pyrimidines/pharmacology ; Tretinoin
Czasopismo naukowe
Tytuł :
Phase II study of tazemetostat for relapsed or refractory B-cell non-Hodgkin lymphoma with EZH2 mutation in Japan.
Autorzy :
Izutsu K; Department of Hematology, National Cancer Center Hospital, Tokyo, Japan.
Ando K; Department of Hematology and Oncology, Tokai University School of Medicine, Isehara, Japan.
Nishikori M; Department of Hematology and Oncology, Kyoto University, Kyoto, Japan.
Shibayama H; Department of Hematology and Oncology, Osaka University Hospital, Osaka, Japan.
Teshima T; Department of Hematology, Hokkaido University Faculty of Medicine, Sapporo, Japan.
Kuroda J; Division of Hematology and Oncology, Kyoto Prefectural University of Medicine, Kyoto, Japan.
Kato K; Department of Hematology and Oncology, Kyushu University Hospital, Fukuoka, Japan.
Imaizumi Y; Department of Hematology, Nagasaki University Hospital, Nagasaki, Japan.
Nosaka K; Department of Hematology, Rheumatology, and Infectious Diseases, Kumamoto University, Kumamoto, Japan.
Sakai R; Department of Hematology and Medical Oncology, Kanagawa Cancer Center, Yokohama, Japan.
Hojo S; Eisai Co., Ltd., Tokyo, Japan.
Nakanishi T; Eisai Co., Ltd., Tokyo, Japan.
Rai S; Department of Hematology and Rheumatology, Kindai University Hospital, Osaka, Japan.
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Źródło :
Cancer science [Cancer Sci] 2021 Sep; Vol. 112 (9), pp. 3627-3635. Date of Electronic Publication: 2021 Jul 14.
Typ publikacji :
Clinical Trial, Phase II; Journal Article; Multicenter Study
MeSH Terms :
Mutation*
Antineoplastic Agents/*adverse effects
Benzamides/*adverse effects
Biphenyl Compounds/*adverse effects
Enhancer of Zeste Homolog 2 Protein/*genetics
Lymphoma, Follicular/*drug therapy
Lymphoma, Follicular/*genetics
Lymphoma, Large B-Cell, Diffuse/*drug therapy
Lymphoma, Large B-Cell, Diffuse/*genetics
Morpholines/*adverse effects
Pyridones/*adverse effects
Aged ; Aged, 80 and over ; Antineoplastic Agents/administration & dosage ; Benzamides/administration & dosage ; Biphenyl Compounds/administration & dosage ; Cohort Studies ; Enhancer of Zeste Homolog 2 Protein/antagonists & inhibitors ; Female ; Humans ; Japan/epidemiology ; Lymphoma, Follicular/epidemiology ; Lymphoma, Large B-Cell, Diffuse/epidemiology ; Male ; Middle Aged ; Morpholines/administration & dosage ; Progression-Free Survival ; Pyridones/administration & dosage ; Recurrence
Czasopismo naukowe
Tytuł :
Combination of Chidamide-Mediated Epigenetic Modulation with Immunotherapy: Boosting Tumor Immunogenicity and Response to PD-1/PD-L1 Blockade.
Autorzy :
Tu K; Tongji School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Yu Y; Tongji School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Wang Y; Tongji School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Yang T; Tongji School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Hu Q; Tongji School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Qin X; Tongji School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Tu J; Department of Oncology, Tongji Hospital, Huazhong University of Science and Technology, Wuhan 430030, China.
Yang C; Tongji School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Kong L; Tongji School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
Zhang Z; Department of Oncology, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, 1095 Jiefang Avenue, Wuhan 430030, Hubei, China.; National Engineering Research Center for Nanomedicine, Huazhong University of Science and Technology, Wuhan 430030, China.; Hubei Engineering Research Center for Novel Drug Delivery System, Huazhong University of Science and Technology, Wuhan 430030, China.
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Źródło :
ACS applied materials & interfaces [ACS Appl Mater Interfaces] 2021 Aug 25; Vol. 13 (33), pp. 39003-39017. Date of Electronic Publication: 2021 Aug 16.
Typ publikacji :
Journal Article
MeSH Terms :
Acetamides/*chemistry
Aminopyridines/*chemistry
Antineoplastic Agents/*pharmacology
Benzamides/*chemistry
Drug Carriers/*chemistry
Immune Checkpoint Inhibitors/*chemistry
Pyridines/*chemistry
Triple Negative Breast Neoplasms/*drug therapy
Triple Negative Breast Neoplasms/*immunology
Acetamides/pharmacology ; Aminopyridines/pharmacology ; Animals ; Benzamides/pharmacology ; Biocompatible Materials/chemistry ; Cell Line, Tumor ; Combined Modality Therapy/methods ; Drug Liberation ; Epigenesis, Genetic/drug effects ; Female ; Humans ; Immune Checkpoint Inhibitors/pharmacology ; Immunotherapy/methods ; Liposomes/chemistry ; Mice ; Mice, Inbred BALB C ; Pyridines/pharmacology ; Small Molecule Libraries/chemistry ; Tissue Distribution ; Treatment Outcome
Czasopismo naukowe
Tytuł :
Comparison of the drug-drug interactions potential of ibrutinib and acalabrutinib via inhibition of UDP-glucuronosyltransferase.
Autorzy :
Wang X; School of Life and Pharmaceutical Sciences, Dalian University of Technology, Panjin 124221, China.
Wang Z; School of Life and Pharmaceutical Sciences, Dalian University of Technology, Panjin 124221, China.
Fan X; School of Life and Pharmaceutical Sciences, Dalian University of Technology, Panjin 124221, China.
Yan M; School of Life and Pharmaceutical Sciences, Dalian University of Technology, Panjin 124221, China.
Jiang L; School of Life and Pharmaceutical Sciences, Dalian University of Technology, Panjin 124221, China.
Xia Y; School of Life and Pharmaceutical Sciences, Dalian University of Technology, Panjin 124221, China.
Cao J; Department of Occupational and Environmental Health, Dalian Medical University, Dalian 116044, China. Electronic address: .
Liu Y; School of Life and Pharmaceutical Sciences, Dalian University of Technology, Panjin 124221, China. Electronic address: .
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Źródło :
Toxicology and applied pharmacology [Toxicol Appl Pharmacol] 2021 Aug 01; Vol. 424, pp. 115595. Date of Electronic Publication: 2021 May 24.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Adenine/*analogs & derivatives
Benzamides/*pharmacokinetics
Glucuronosyltransferase/*antagonists & inhibitors
Piperidines/*pharmacokinetics
Pyrazines/*pharmacokinetics
Adenine/chemistry ; Adenine/pharmacokinetics ; Benzamides/chemistry ; Drug Interactions ; Humans ; Isoenzymes ; Molecular Structure ; Piperidines/chemistry ; Pyrazines/chemistry
Czasopismo naukowe
Tytuł :
Indirect Comparison of Darolutamide versus Apalutamide and Enzalutamide for Nonmetastatic Castration-Resistant Prostate Cancer.
Autorzy :
Halabi S; Duke University, Durham, North Carolina.
Jiang S; Bayer, Whippany, New Jersey.
Terasawa E; Analysis Group, Inc., New York, New York.
Garcia-Horton V; Analysis Group, Inc., New York, New York.
Ayyagari R; Analysis Group, Inc., Boston, Massachusetts.
Waldeck AR; Bayer, Whippany, New Jersey.
Shore N; Carolina Urologic Research Center, Myrtle Beach, South Carolina.
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Źródło :
The Journal of urology [J Urol] 2021 Aug; Vol. 206 (2), pp. 298-307. Date of Electronic Publication: 2021 Apr 05.
Typ publikacji :
Clinical Trial, Phase III; Journal Article; Randomized Controlled Trial
MeSH Terms :
Benzamides/*adverse effects
Nitriles/*adverse effects
Phenylthiohydantoin/*adverse effects
Prostatic Neoplasms, Castration-Resistant/*drug therapy
Pyrazoles/*adverse effects
Thiohydantoins/*adverse effects
Accidental Falls/statistics & numerical data ; Androgen Receptor Antagonists/administration & dosage ; Androgen Receptor Antagonists/adverse effects ; Benzamides/administration & dosage ; Cognitive Dysfunction/chemically induced ; Dizziness/chemically induced ; Exanthema/chemically induced ; Fatigue/chemically induced ; Fractures, Spontaneous/chemically induced ; Humans ; Male ; Middle Aged ; Nitriles/administration & dosage ; Phenylthiohydantoin/administration & dosage ; Prostatic Neoplasms, Castration-Resistant/mortality ; Pyrazoles/administration & dosage ; Thiohydantoins/administration & dosage
Czasopismo naukowe
Tytuł :
Enzalutamide With Radiation Therapy for Intermediate-Risk Prostate Cancer: A Phase 2 Study.
Autorzy :
Kaplan I; Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts. Electronic address: .
Bubley GJ; Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts.
Bhatt RS; Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts.
Taplin ME; Department of Medical Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, Massachusetts.
Dowling S; Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts.
Mahoney K; Beth Israel Deaconess Medical Center, Harvard Medical School, Boston, Massachusetts.
Werner E; Department of Biostatics, Dana-Farber Cancer Institute, Harvard Medical School, Boston, Massachusetts.
Nguyen P; Department of Radiation Oncology, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts.
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Źródło :
International journal of radiation oncology, biology, physics [Int J Radiat Oncol Biol Phys] 2021 Aug 01; Vol. 110 (5), pp. 1416-1422. Date of Electronic Publication: 2021 Feb 23.
Typ publikacji :
Clinical Trial, Phase II; Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Androgen Antagonists/*therapeutic use
Benzamides/*therapeutic use
Nitriles/*therapeutic use
Phenylthiohydantoin/*therapeutic use
Prostate-Specific Antigen/*blood
Prostatic Neoplasms/*drug therapy
Prostatic Neoplasms/*radiotherapy
Androgen Antagonists/adverse effects ; Androgens/blood ; Benzamides/adverse effects ; Body Composition/drug effects ; Body Fat Distribution ; Gynecomastia/chemically induced ; Humans ; Hypertension/chemically induced ; Male ; Nitriles/adverse effects ; Phenylthiohydantoin/adverse effects ; Prostatic Neoplasms/blood ; Prostatic Neoplasms/pathology ; Risk ; Testosterone/blood ; Time Factors
Czasopismo naukowe
Tytuł :
Design and synthesis of Grp94 selective inhibitors based on Phe199 induced fit mechanism and their anti-inflammatory effects.
Autorzy :
Xu S; State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Guo A; State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Chen NN; State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Dai W; State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Yang HA; State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Xie W; State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
Wang M; State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China.
You QD; State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China. Electronic address: .
Xu XL; State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Nov 05; Vol. 223, pp. 113604. Date of Electronic Publication: 2021 Jun 09.
Typ publikacji :
Journal Article
MeSH Terms :
Alkynes/*therapeutic use
Anti-Inflammatory Agents/*therapeutic use
Benzamides/*therapeutic use
Colitis, Ulcerative/*drug therapy
Membrane Glycoproteins/*antagonists & inhibitors
Alkynes/chemical synthesis ; Alkynes/metabolism ; Alkynes/pharmacokinetics ; Animals ; Anti-Inflammatory Agents/chemical synthesis ; Anti-Inflammatory Agents/metabolism ; Anti-Inflammatory Agents/pharmacokinetics ; Benzamides/chemical synthesis ; Benzamides/metabolism ; Benzamides/pharmacokinetics ; Colitis, Ulcerative/pathology ; Colon/drug effects ; Colon/pathology ; HCT116 Cells ; Humans ; Male ; Membrane Glycoproteins/metabolism ; Mice, Inbred C57BL ; Microsomes, Liver/metabolism ; Molecular Docking Simulation ; Molecular Structure ; Protein Binding ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Discovery of Novel 2,4-Dianilinopyrimidine Derivatives Containing 4-(Morpholinomethyl)phenyl and N -Substituted Benzamides as Potential FAK Inhibitors and Anticancer Agents.
Autorzy :
Han C; Department of Chemistry, Changzhi University, Changzhi 046011, China.
Shen K; Department of Public Health and Preventive Medicine, Changzhi Medical College, Changzhi 046011, China.
Wang S; Department of Chemistry, Changzhi University, Changzhi 046011, China.
Wang Z; Department of Chemistry, Changzhi University, Changzhi 046011, China.
Su F; Department of Chemistry, Changzhi University, Changzhi 046011, China.
Wu X; Department of Chemistry, Changzhi University, Changzhi 046011, China.
Hu X; Department of Chemistry, Changzhi University, Changzhi 046011, China.
Li M; Department of Chemistry, Changzhi University, Changzhi 046011, China.
Han J; School of Chemistry and Materials Science, Jiangsu Normal University, Xuzhou 221116, China.
Wu L; Department of Chemistry, Changzhi University, Changzhi 046011, China.
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Źródło :
Molecules (Basel, Switzerland) [Molecules] 2021 Jul 09; Vol. 26 (14). Date of Electronic Publication: 2021 Jul 09.
Typ publikacji :
Journal Article
MeSH Terms :
Benzamides/*pharmacology
Focal Adhesion Protein-Tyrosine Kinases/*antagonists & inhibitors
Phenols/*pharmacology
Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; Benzamides/chemistry ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Drug Design ; Drug Screening Assays, Antitumor/methods ; Focal Adhesion Protein-Tyrosine Kinases/chemistry ; Humans ; Molecular Docking Simulation ; Molecular Structure ; Morpholines/pharmacology ; Neoplasms/drug therapy ; Phenols/chemistry ; Protein Kinase Inhibitors/pharmacology ; Pyrimidines/chemistry ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Second-Generation Dual FXR/sEH Modulators with Optimized Pharmacokinetics.
Autorzy :
Helmstädter M; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, 60438 Frankfurt, Germany.
Kaiser A; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, 60438 Frankfurt, Germany.
Brunst S; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, 60438 Frankfurt, Germany.
Schmidt J; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, 60438 Frankfurt, Germany.
Ronchetti R; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, 60438 Frankfurt, Germany.
Weizel L; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, 60438 Frankfurt, Germany.
Proschak E; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, 60438 Frankfurt, Germany.
Merk D; Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, 60438 Frankfurt, Germany.
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Źródło :
Journal of medicinal chemistry [J Med Chem] 2021 Jul 08; Vol. 64 (13), pp. 9525-9536. Date of Electronic Publication: 2021 Jun 24.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Benzamides/*pharmacology
Enzyme Inhibitors/*pharmacology
Epoxide Hydrolases/*antagonists & inhibitors
Receptors, Cytoplasmic and Nuclear/*metabolism
Animals ; Benzamides/chemical synthesis ; Benzamides/chemistry ; Cell Survival/drug effects ; Dose-Response Relationship, Drug ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Epoxide Hydrolases/metabolism ; Hep G2 Cells ; Humans ; Microsomes, Liver/chemistry ; Microsomes, Liver/metabolism ; Molecular Structure ; Rats ; Rats, Sprague-Dawley ; Receptors, Cytoplasmic and Nuclear/genetics ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo.
Autorzy :
Liu YM; School of Pharmacy, College of Pharmacy, Taipei Medical University, 250 Wuxing Street, Taipei, 11031, Taiwan; Biomedical Commercialization Center, Taipei Medical University, Taipei, 11031, Taiwan.
Tu HJ; Graduate Institute of Cancer Molecular Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, 11031, Taiwan.
Wu CH; Pharmacological Institute, College of Medicine, National Taiwan University, Taipei, Taiwan.
Lai MJ; Biomedical Commercialization Center, Taipei Medical University, Taipei, 11031, Taiwan; Ph.D. Program in Drug Discovery and Development Industry, College of Pharmacy, Taipei Medical University, Taipei, 11031, Taiwan.
Yu SC; School of Pharmacy, College of Pharmacy, Taipei Medical University, 250 Wuxing Street, Taipei, 11031, Taiwan.
Chao MW; Graduate Institute of Cancer Molecular Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, 11031, Taiwan.
Wu YW; Graduate Institute of Cancer Molecular Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, 11031, Taiwan.
Teng CM; Pharmacological Institute, College of Medicine, National Taiwan University, Taipei, Taiwan.
Pan SL; Biomedical Commercialization Center, Taipei Medical University, Taipei, 11031, Taiwan; Graduate Institute of Cancer Molecular Biology and Drug Discovery, College of Medical Science and Technology, Taipei Medical University, Taipei, 11031, Taiwan; Ph.D. Program in Drug Discovery and Development Industry, College of Pharmacy, Taipei Medical University, Taipei, 11031, Taiwan. Electronic address: .
Liou JP; School of Pharmacy, College of Pharmacy, Taipei Medical University, 250 Wuxing Street, Taipei, 11031, Taiwan; Biomedical Commercialization Center, Taipei Medical University, Taipei, 11031, Taiwan; Ph.D. Program in Drug Discovery and Development Industry, College of Pharmacy, Taipei Medical University, Taipei, 11031, Taiwan. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Jul 05; Vol. 219, pp. 113428. Date of Electronic Publication: 2021 Apr 06.
Typ publikacji :
Journal Article
MeSH Terms :
Benzamides/*chemistry
HSP90 Heat-Shock Proteins/*antagonists & inhibitors
Resorcinols/*chemistry
Afatinib/therapeutic use ; Animals ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/metabolism ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Benzamides/metabolism ; Benzamides/pharmacology ; Benzamides/therapeutic use ; Cell Cycle Checkpoints/drug effects ; Cell Line ; Cell Membrane Permeability/drug effects ; Cell Movement/drug effects ; Cell Proliferation/drug effects ; Drug Design ; Drug Screening Assays, Antitumor ; Drug Stability ; ErbB Receptors/metabolism ; HSP90 Heat-Shock Proteins/metabolism ; Half-Life ; Humans ; Lung Neoplasms/drug therapy ; Lung Neoplasms/pathology ; Rats ; Transplantation, Heterologous
Czasopismo naukowe
Tytuł :
Discovery of N-substituted sulfamoylbenzamide derivatives as novel inhibitors of STAT3 signaling pathway based on Niclosamide.
Autorzy :
Wang X; Department of Colorectal Surgery, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China.
Wu K; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China.
Fang L; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China.
Yang X; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China.
Zheng N; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China.
Du Z; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China.
Lu Y; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China.
Xie Z; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China.
Liu Z; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China.
Zuo Z; Department of Colorectal Surgery, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China. Electronic address: .
Ye F; Department of Colorectal Surgery, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China; School of Pharmaceutical Science, Wenzhou Medical University, Wenzhou, Zhejiang, 325035, China. Electronic address: .
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Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2021 Jun 05; Vol. 218, pp. 113362. Date of Electronic Publication: 2021 Mar 17.
Typ publikacji :
Journal Article
MeSH Terms :
Drug Discovery*
Benzamides/*pharmacology
Niclosamide/*pharmacology
STAT3 Transcription Factor/*antagonists & inhibitors
Benzamides/chemical synthesis ; Benzamides/chemistry ; Dose-Response Relationship, Drug ; Humans ; Molecular Structure ; Niclosamide/chemical synthesis ; Niclosamide/chemistry ; STAT3 Transcription Factor/metabolism ; Signal Transduction/drug effects ; Structure-Activity Relationship
Czasopismo naukowe
Tytuł :
Safety and antitumor activity of acalabrutinib for relapsed/refractory B-cell malignancies: A Japanese phase I study.
Autorzy :
Izutsu K; National Cancer Center Hospital, Tokyo, Japan.
Ando K; Tokai University Hospital, Isehara, Japan.
Ennishi D; Okayama University Hospital, Okayama, Japan.
Shibayama H; Osaka University Hospital, Osaka, Japan.
Suzumiya J; Shimane University Hospital, Izumo, Japan.
Yamamoto K; Aichi Cancer Center Hospital, Nagoya, Japan.
Ichikawa S; Tohoku University Hospital, Sendai, Japan.
Kato K; Kyushu University Hospital, Fukuoka, Japan.
Kumagai K; Chiba Cancer Center, Chiba, Japan.
Patel P; Acerta Pharma, South San Francisco, CA, USA.
Iizumi S; AstraZeneca K.K., Tokyo, Japan.
Hayashi N; AstraZeneca K.K, Osaka, Japan.
Kawasumi H; AstraZeneca K.K., Tokyo, Japan.
Murayama K; AstraZeneca K.K, Osaka, Japan.
Nagai H; National Hospital Organization Nagoya Medical Center, Nagoya, Japan.
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Źródło :
Cancer science [Cancer Sci] 2021 Jun; Vol. 112 (6), pp. 2405-2415. Date of Electronic Publication: 2021 May 07.
Typ publikacji :
Clinical Trial, Phase I; Journal Article; Multicenter Study
MeSH Terms :
Antineoplastic Agents/*administration & dosage
Benzamides/*administration & dosage
Leukemia, Lymphocytic, Chronic, B-Cell/*drug therapy
Lymphoma, Mantle-Cell/*drug therapy
Neoplasm Recurrence, Local/*drug therapy
Pyrazines/*administration & dosage
Aged ; Aged, 80 and over ; Antineoplastic Agents/adverse effects ; Antineoplastic Agents/pharmacokinetics ; Benzamides/adverse effects ; Benzamides/pharmacokinetics ; Drug Administration Schedule ; Female ; Headache/chemically induced ; Headache/epidemiology ; Humans ; Japan ; Leukemia, Lymphocytic, Chronic, B-Cell/blood ; Lymphoma, Mantle-Cell/blood ; Male ; Middle Aged ; Neoplasm Recurrence, Local/blood ; Purpura/chemically induced ; Purpura/epidemiology ; Pyrazines/adverse effects ; Pyrazines/pharmacokinetics ; Survival Analysis ; Treatment Outcome
Czasopismo naukowe
Tytuł :
Effect of a change in lasmiditan dose on efficacy and safety in patients with migraine.
Autorzy :
Clemow DB; Eli Lilly and Company, Indianapolis, IN, USA.
Hochstetler HM
Dong Y; Eli Lilly and Company, Indianapolis, IN, USA.
Hauck P; Eli Lilly and Company, Indianapolis, IN, USA.
Peres MFP; Institute of Psychiatry, University of Sao Paulo, Sao Paulo, Brazil.; Hospital Albert Einstein, Sao Paulo, Brazil.
Ailani J; MedStar Georgetown Headache Center, Georgetown University, Washington, DC, USA.
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Źródło :
Postgraduate medicine [Postgrad Med] 2021 May; Vol. 133 (4), pp. 449-459. Date of Electronic Publication: 2021 Mar 17.
Typ publikacji :
Clinical Trial, Phase III; Journal Article; Randomized Controlled Trial
MeSH Terms :
Benzamides/*therapeutic use
Migraine Disorders/*drug therapy
Piperidines/*therapeutic use
Pyridines/*therapeutic use
Serotonin Receptor Agonists/*therapeutic use
Adult ; Benzamides/administration & dosage ; Benzamides/adverse effects ; Dose-Response Relationship, Drug ; Double-Blind Method ; Female ; Humans ; Male ; Middle Aged ; Piperidines/administration & dosage ; Piperidines/adverse effects ; Pyridines/administration & dosage ; Pyridines/adverse effects ; Serotonin Receptor Agonists/administration & dosage ; Serotonin Receptor Agonists/adverse effects ; Severity of Illness Index
Czasopismo naukowe
Tytuł :
A drug safety evaluation of enzalutamide to treat advanced prostate cancer.
Autorzy :
Saad F; Department of Surgery/Urology, University of Montreal Hospital Center (CHUM), Montreal, Canada.
Hamilou Z; Department of Medicine/Medical Oncology, University of Montreal Hospital Center (CHUM), Montreal, Canada.
Lattouf JB; Department of Surgery/Urology, University of Montreal Hospital Center (CHUM), Montreal, Canada.
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Źródło :
Expert opinion on drug safety [Expert Opin Drug Saf] 2021 Jul; Vol. 20 (7), pp. 741-749. Date of Electronic Publication: 2021 Jun 11.
Typ publikacji :
Journal Article; Review
MeSH Terms :
Antineoplastic Agents/*administration & dosage
Benzamides/*administration & dosage
Nitriles/*administration & dosage
Phenylthiohydantoin/*administration & dosage
Prostatic Neoplasms/*drug therapy
Androgen Receptor Antagonists/administration & dosage ; Androgen Receptor Antagonists/adverse effects ; Antineoplastic Agents/adverse effects ; Benzamides/adverse effects ; Humans ; Male ; Nitriles/adverse effects ; Phenylthiohydantoin/adverse effects ; Prostatic Neoplasms/pathology ; Quality of Life
Czasopismo naukowe
Tytuł :
Molecular Determinants Underlying Delta Selective Compound 2 Activity at δ -Containing GABA A Receptors.
Autorzy :
Falk-Petersen CB; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
Rostrup F; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
Löffler R; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
Buchleithner S; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
Harpsøe K; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
Gloriam DE; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
Frølund B; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark.
Wellendorph P; Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark .
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Źródło :
Molecular pharmacology [Mol Pharmacol] 2021 Jul; Vol. 100 (1), pp. 46-56. Date of Electronic Publication: 2021 May 14.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
MeSH Terms :
Benzamides/*pharmacology
Imidazoles/*pharmacology
Mutagenesis, Site-Directed/*methods
Receptors, GABA-A/*chemistry
Receptors, GABA-A/*metabolism
Allosteric Regulation ; Benzamides/chemistry ; Binding Sites ; Diazepam/pharmacology ; Etomidate/pharmacology ; HEK293 Cells ; Humans ; Imidazoles/chemistry ; Models, Molecular ; Molecular Conformation ; Molecular Docking Simulation ; Multiprotein Complexes/chemistry ; Multiprotein Complexes/metabolism ; Protein Binding ; Protein Domains ; Receptors, GABA-A/genetics
Czasopismo naukowe
Tytuł :
FDA-approved 5-HT 1F receptor agonist lasmiditan induces mitochondrial biogenesis and enhances locomotor and blood-spinal cord barrier recovery after spinal cord injury.
Autorzy :
Simmons EC; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, AZ, United States of America; Department of Neurosciences, College of Medicine, University of Arizona, Tucson, AZ, United States of America. Electronic address: .
Scholpa NE; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, AZ, United States of America; Southern Arizona VA Health Care System, Tucson, AZ, United States of America. Electronic address: .
Schnellmann RG; Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson, AZ, United States of America; Department of Neurosciences, College of Medicine, University of Arizona, Tucson, AZ, United States of America; College of Pharmacy, University of Arizona, Tucson, AZ, United States of America; Southern Arizona VA Health Care System, Tucson, AZ, United States of America; Southwest Environmental Health Science Center, University of Arizona, Tucson, AZ, United States of America; Center for Innovation in Brain Science, University of Arizona, Tucson, AZ, United States of America. Electronic address: .
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Źródło :
Experimental neurology [Exp Neurol] 2021 Jul; Vol. 341, pp. 113720. Date of Electronic Publication: 2021 Apr 10.
Typ publikacji :
Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, Non-P.H.S.
MeSH Terms :
Organelle Biogenesis*
Benzamides/*therapeutic use
Blood-Brain Barrier/*drug effects
Locomotion/*drug effects
Mitochondria/*drug effects
Piperidines/*therapeutic use
Pyridines/*therapeutic use
Spinal Cord Injuries/*drug therapy
Animals ; Benzamides/pharmacology ; Blood-Brain Barrier/pathology ; Blood-Brain Barrier/physiopathology ; Female ; Locomotion/physiology ; Mice ; Mice, Inbred C57BL ; Mitochondria/physiology ; Piperidines/pharmacology ; Pyridines/pharmacology ; Recovery of Function/drug effects ; Recovery of Function/physiology ; Serotonin Receptor Agonists/pharmacology ; Serotonin Receptor Agonists/therapeutic use ; Spinal Cord/drug effects ; Spinal Cord/pathology ; Spinal Cord/physiology ; Spinal Cord Injuries/pathology ; Spinal Cord Injuries/physiopathology
Czasopismo naukowe

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