[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: Juan Feng, Peng Xie, Zhi-Jie Weng, Zheng Yan, Nan Wang, Jian-Qi Li
• Journal: Yao xue xue bao = Acta pharmaceutica Sinica (Yao Xue Xue Bao) Vol. 44 Issue 6 Pg. 603-8 (Jun 2009) ISSN: 0513-4870 [Print] China
• PMID: 19806890 (Publication Type: English Abstract, Journal Article)

Chemical References

• Antineoplastic Agents
• Benzamides

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Benzamides (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Humans