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[Synthesis and anti-tumor activities of N-substituted benzamide derivatives].

Authors :
Feng J
Xie P
Weng ZJ
Yan Z
Wang N
Li JQ
Source :
Yao xue xue bao = Acta pharmaceutica Sinica [Yao Xue Xue Bao] 2009 Jun; Vol. 44 (6), pp. 603-8.
Publication Year :
2009

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.

Details

Language :
Chinese
ISSN :
0513-4870
Volume :
44
Issue :
6
Database :
MEDLINE
Journal :
Yao xue xue bao = Acta pharmaceutica Sinica
Publication Type :
Academic Journal
Accession number :
19806890