Synthesis and anti-tumor activities of N-substituted benzamide derivatives.
- Author:
Juan FENG
1
;
Peng XIE
;
Zhi-Jie WENG
;
Zheng YAN
;
Nan WANG
;
Jian-Qi LI
Author Information
1. Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Benzamides;
chemical synthesis;
chemistry;
pharmacology;
Cell Line, Tumor;
Humans
- From:
Acta Pharmaceutica Sinica
2009;44(6):603-608
- CountryChina
- Language:Chinese
-
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.
