title: [Synthesis and anti-tumor activities of N-substituted benzamide derivatives].
abstract: To explore novel histone deacetylase (HDACs) inhibitors with anti-tumor activity, MS-275, a HDACs inhibitor, was prepared and used as a lead compound to design new N-substituted benzamide derivatives. MS-275 and eleven target compounds were obtained, and their structures were confirmed by 1H NMR and HR-MS individually. The results showed that the activity of compound 9d was equal to MS-275 in HDACs inhibition tests in vitro and worthy of further investigation. Compound 5c, 5d and 9c displayed obvious dose-effect relationship, which possessed moderate HDACs inhibitory activities. Ten compounds except 9e had selective inhibitory activities on Hut78.
authors.affiliation: Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
authors.forename: Juan
authors.initials: J
authors.lastname: Feng
authors.forename: Peng
authors.initials: P
authors.lastname: Xie
authors.forename: Zhi-Jie
authors.initials: ZJ
authors.lastname: Weng
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yan
authors.forename: Nan
authors.initials: N
authors.lastname: Wang
authors.forename: Jian-Qi
authors.initials: JQ
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001549:Benzamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D006801:Humans
chemical_list: D000970:Antineoplastic Agents; D001549:Benzamides