Design, synthesis and cytotoxicity screening of new synthesized pyrimidine-5-carbonitrile derivatives showing marked apoptotic effect

Journal of Molecular Structure(2022)

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摘要
•A new series of pyrimidine-5-carbonitriles have been designed and synthesized.•Potent VEGFR-2 inhibitory activity correlated cytotoxicity of compound 5a.•Compounds 5a and 6c showed significant cytotoxic activity against HepG2 cells•Compounds 5a and 6c arrested the cell cycle at G2/M phase and induced apoptosis by increasing pre-G1 phase•The pro-apoptotic activity for compounds 5a and 6c were due to up-regulation of p53, Bax and downregulation of Bcl2.
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关键词
Pyrimidine,Anticancer,Cell cycle analysis,VEGFR-2,Bax,Bcl2,p53, Caspase 3/7
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