Synthesis and anticancer activities of thieno[3,2-d]pyrimidines as novel HDAC inhibitors

Bioorganic & Medicinal Chemistry
2014.0

Abstract

A series of thieno[3,2-d]pyrimidines bearing a hydroxamic acid moiety as novel HDAC inhibitors were designed and synthesized. The structures of the new synthesized compounds were confirmed using IR, (1)H, (13)C NMR spectrum. Compounds 11-13 showed potent inhibitory activities against HDACs with IC₅₀ values at 0.38, 0.49 and 0.61 μM. Most of target compounds displayed strong anti-proliferative activity by a MTT assay on three human cancer cell lines including HCT-116, MCF-7 and HeLa. Compound 11, having potent inhibitory activities against HDACs, induced apoptosis and G2/M cell cycle arrest in HCT-116 cell line.

DOI： 10.1016/j.bmc.2013.11.021

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