期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 83, 期 -, 页码 155-166出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.06.027
关键词
Pyrido[2,3-d]pyrimidine; Pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidine; Antitumor activity; Apoptosis; Cell cycle arrest
资金
- Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Egypt
- Deanship of Scientific Research at King Saud University [RGP-VPP-321]
New series of 2-(2-arylidenehydrazinyl)pyrido[2,3-djpyrimidines 5a-e and pyrido[2,3-d][1,2,4]triazolo [4,3-a]pyrimidines 6-15 were synthesized and evaluated for their cytotoxic activity against two cancer cell lines, namely PC-3 prostate cancer and A-549 lung cancer. Some of the tested compounds displayed high growth inhibitory activity against PC-3 cells. Whereas, compounds 5b and 15f showed relatively potent antitumor activity against PC-3 and A-549 cell lines. In particular, 4-(3-acetyl-5-oxo-6-phenyl-8-(thiophen-2-yl)pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-1(5H)-yl)benzenesulfonamide 15f exhibited superior antitumor activity against both cell lines at submicromolar level (IC50 = 0.36, 0.41 mu M, respectively). Moreover, the potential mechanisms of the cytotoxic activity of the promising compound 15f on the more sensitive cell line PC-3 were studied. The data indicated that 15f was able to cause cell cycle arrest at least partly through enhancing the expression level of the cell cycle inhibitor p21 and induced cancer cell apoptosis via caspase-3 dependent pathway. (C) 2014 Elsevier Masson SAS. All rights reserved.
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