Bhagwanrao, P. V. <br/><br/>
Synthesis and biological evaluation of 2-phenylpyrido[2,3-D] pyrimidine derivatives as cyclin-dependent kinase H(CDK) inhibitors 

 - Vol.56(5), May 
 - Mumbai  Indian Drug Manufacture's Association - IDMA  2019 
 - 50-58p. 
<br/><br/> 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. 
<br/><br/><label>Subjects--Topical Terms: </label><br/>PHARMACEUTICS