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Yao xue xue bao = Acta pharmaceutica Sinica 2009-Jun

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

Samo registrirani uporabniki lahko prevajajo članke
Prijava / prijava
Povezava se shrani v odložišče
Juan Feng
Peng Xie
Zhi-Jie Weng
Zheng Yan
Nan Wang
Jian-Qi Li

Ključne besede

Povzetek

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.

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