Synthesis and biological evaluation of 2-phenylpyrido[2,3-D] pyrimidine derivatives as cyclin-dependent kinase H(CDK) inhibitors
By: Bhagwanrao, P. V.
Contributor(s): Ingole, P. G.
Publisher: Mumbai Indian Drug Manufacture's Association - IDMA 2019Edition: Vol.56(5), May.Description: 50-58p.Subject(s): PHARMACEUTICSOnline resources: Click here In: Indian drugsSummary: 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.Item type | Current location | Call number | Status | Date due | Barcode | Item holds |
---|---|---|---|---|---|---|
Articles Abstract Database | School of Pharmacy Archieval Section | Not for loan | 2020653 |
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.
There are no comments for this item.