[Synthesis and anti-tumor activities of N-substituted benzamide derivatives].
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.
Feng
Juan
J
Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
Xie
Peng
P
Weng
Zhi-Jie
ZJ
Yan
Zheng
Z
Wang
Nan
N
Li
Jian-Qi
JQ
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
D000970:Antineoplastic Agents; D001549:Benzamides