Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors

• Main Authors: Yumei Zhou, Huaqing Cui, Xiaoming Yu, Tao Peng, Gang Wang, Xiaoxue Wen, Yunbo Sun, Shuchen Liu, Shouguo Zhang, Liming Hu, Lin Wang
• Format: Article
• Language: English
• Published: MDPI AG 2017-08-01
• Series: Molecules
• Subjects: benzofuran; sulfoxide; sulfone; selective SIRT2 inhibitor
• Online Access: https://www.mdpi.com/1420-3049/22/8/1348
• ISSN: 1420-3049

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.