期刊
FUTURE MEDICINAL CHEMISTRY
卷 11, 期 18, 页码 2395-2414出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2019-0050
关键词
anticancer; apoptosis; CDK; cell cycle; pyrido[2,3-d]pyrimidine
Aim: Due to emergence of resistance to available anticancer agents, there is a need to search for new cytotoxic agents. Methods: Pyrido[2,3-d]pyrimidines (4-6) and their tricyclic derivatives (7-13) were prepared and screened for their cytotoxicity against breast MCF-7, prostate PC-3 and lung A-549 cancer cell lines as well as normal fibroblasts WI-38. Results: The most active compounds were 6b, 6e and 8d compared with doxorubicin. Moreover, compounds 6b and 8d induced apoptosis in PC-3 and MCF-7, respectively via activation of CASP3 (in PC-3 only), Bax, p53 and down regulation of Bcl2 in addition to CDK4/6 inhibition. Conclusion: Pyrido[2,3-d]pyrimidine represents an important core for discovery of new potent cytotoxic agents acting on the cell cycle via apoptosis induction through either intrinsic or extrinsic pathways. [GRAPHICS] .
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