Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors

Molecules

Yumei Zhou¹  Liming Hu¹  Lin Wang¹  Xiaoming Yu²  Huaqing Cui²  Yunbo Sun³  Shuchen Liu³  Gang Wang³  Xiaoxue Wen³  Shouguo Zhang³  Tao Peng³ 

[1] College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China;Institute of MateriaMedica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China;Institute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China;

关键词: benzofuran;    sulfoxide;    sulfone;    selective SIRT2 inhibitor;   

DOI  :  10.3390/molecules22081348

来源: DOAJ

【 摘 要 】

A series of benzofuran derivatives were designed and synthesized, and their inhibitory activites were measured against the SIRT1–3. The enzymatic assay showed that all the compounds showed certain anti-SIRT2 activity and selective over SIRT1 and SIRT3 with IC50 (half maximal inhibitory concentration) values at the micromolar level. The preliminary structure–activity relationships were analyzed and the binding features of compound 7e (IC50 3.81 µM) was predicted using the CDOCKER program. The results of this research could provide informative guidance for further optimizing benzofuran derivatives as potent SIRT2 inhibitors.

【 授权许可】

Unknown