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Tytuł pozycji:

Synthesis of novel substituted purine derivatives and identification of the cell death mechanism.

Tytuł :
Synthesis of novel substituted purine derivatives and identification of the cell death mechanism.
Autorzy :
Demir Z; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Ankara, Turkey.
Guven EB; Department of Molecular Biology and Genetics, Bilkent University, 06800 Ankara, Turkey.
Ozbey S; Department of Engineering Physics, Faculty of Engineering, Hacettepe University, 06800 Beytepe, Ankara, Turkey.
Kazak C; Department of Physics, Faculty of Arts and Sciences, Ondokuz Mayıs University, 55139 Kurupelit, Samsun, Turkey.
Atalay RC; Department of Molecular Biology and Genetics, Bilkent University, 06800 Ankara, Turkey. Electronic address: .
Tuncbilek M; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Ankara, Turkey. Electronic address: .
Pokaż więcej
Źródło :
European journal of medicinal chemistry [Eur J Med Chem] 2015 Jan 07; Vol. 89, pp. 701-20. Date of Electronic Publication: 2014 Oct 30.
Typ publikacji :
Journal Article; Research Support, Non-U.S. Gov't
Język :
English
Imprint Name(s) :
Publication: Paris : Editions Scientifiques Elsevier
Original Publication: Paris, S.E.C.T. [etc.]
MeSH Terms :
Antineoplastic Agents/*chemical synthesis
Antineoplastic Agents/*pharmacology
Purines/*chemistry
Purines/*pharmacology
Antineoplastic Agents/chemistry ; Cell Death/drug effects ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; HCT116 Cells ; Hep G2 Cells ; Humans ; Models, Molecular ; Molecular Structure ; Structure-Activity Relationship ; Tumor Cells, Cultured
Contributed Indexing :
Keywords: Adenine; Cytotoxic activity; Hepatocellular carcinoma; Purine derivatives; Senescence
Substance Nomenclature :
0 (Antineoplastic Agents)
0 (Purines)
W60KTZ3IZY (purine)
Entry Date(s) :
Date Created: 20141203 Date Completed: 20150831 Latest Revision: 20141208
Update Code :
20210623
DOI :
10.1016/j.ejmech.2014.10.080
PMID :
25462277
Czasopismo naukowe
Novel 9-(substituted amino/piperazinoethyl)adenines (4-12), 6-(substituted piperazino/amino)purines (15-27), 9-(p-toluenesulfonyl/cyclopentyl/ethoxycarbonylmethyl)-6-(substituted amino/piperazino)purines (28-34, 36, 37, 38-41) were synthesized and evaluated initially for their cytotoxic activities on liver Huh7, breast T47D and colon HCT116 carcinoma cells. N(6)-(4-Trifluoromethylphenyl)piperazine derivative (17) and its 9-(p-toluene-sulfonyl)/9-cyclopentyl analogues (28, 36) had promising cytotoxic activities. Compounds 17, 28 and 36 were further analysed for their cytotoxicity in a panel of a liver cancer cell lines. The compound 36 had better cytotoxic activities (IC50 ≤ 1 μM) than the nucleobase 5-FU and nucleosides fludarabine, cladribine, and pentostatine on Huh7 cells. Cytotoxicity induced by 36 was later identified as senescence associated cell death by SA-β-Gal assay.
(Copyright © 2014 Elsevier Masson SAS. All rights reserved.)

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