title: 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 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.
authors.affiliation: Institute of Nautical Medicine, Nantong University, 19 Qixiu Road, Nantong 226001, China.
authors.forename: Qiu
authors.initials: Q
authors.lastname: Tan
authors.affiliation: Institute of Nautical Medicine, Nantong University, 19 Qixiu Road, Nantong 226001, China.
authors.forename: Zhitao
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: Institute of Nautical Medicine, Nantong University, 19 Qixiu Road, Nantong 226001, China.
authors.forename: Jie
authors.initials: J
authors.lastname: Hui
authors.affiliation: Institute of Nautical Medicine, Nantong University, 19 Qixiu Road, Nantong 226001, China.
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: Institute of Nautical Medicine, Nantong University, 19 Qixiu Road, Nantong 226001, China. Electronic address: zhulili65@163.com.
authors.forename: Li
authors.initials: L
authors.lastname: Zhu
mesh_terms: D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D056572:Histone Deacetylase Inhibitors; D011743:Pyrimidines
keywords: Anti-proliferative; HDAC; Synthesize; Thieno[3,2-d]pyrimidines