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

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 IC 50 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.