SYNTHESIS AND BIOLOGICAL EVALUATION OF 2-PHENYLPYRIDO[2,3-D] PYRIMIDINE DERIVATIVES AS CYCLIN-DEPENDENT KINASE (CDK) INHIBITORS
Keyword(s):
We report a novel scaffold of 2-phenylpyrido[2,3-d]pyrimidine derivatives designed as structural analogues of dinaciclib. Sixteen derivatives were synthesised and evaluated for their CDK2/5 inhibition activity. Compounds 4-(2-(3-methoxybenzylidene)hydrazineyl)-2-phenylpyrido[2,3-d]pyrimidine (7i) and 4-(2-(3-nitrobenzylidene)hydrazineyl)-2-phenylpyrido[2,3-d]pyrimidine (7n) show promising IC50 and kinase selectivity. These compounds also show moderate anti-proliferative activity in the colon cancer HCT116 and breast cancer MCF7 cell lines. In molecular docking studies with CDK2, compounds 7i and 7nshow binding similar to dinaciclib.
2017 ◽
Vol 27
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pp. 4399-4404
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pp. 954-962