Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors

被引：9

作者：

Zhou, Yumei ^{[1
,2
,3
,4
]}

Cui, Huaqing ^{[3
,4
]}

Yu, Xiaoming ^{[3
,4
]}

Peng, Tao ^{[2
]}

Wang, Gang ^{[2
]}

Wen, Xiaoxue ^{[2
]}

Sun, Yunbo ^{[2
]}

Liu, Shuchen ^{[2
]}

Zhang, Shouguo ^{[2
]}

Hu, Liming ^{[1
]}

Wang, Lin ^{[1
,2
]}

机构：

[1] Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China

[2] Acad Mil Med Sci, Inst Radiat Med, Beijing 100850, Peoples R China

[3] Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China

[4] Peking Union Med Coll, Beijing 100050, Peoples R China

来源：

MOLECULES | 2017年 / 22卷 / 08期

基金：

中国国家自然科学基金;

关键词：

benzofuran; sulfoxide; sulfone; selective SIRT2 inhibitor; PROTEIN DEACETYLASES; MOLECULAR DOCKING; IN-VITRO; 4-(2-HYDROXYARYL)-1,2,3-THIADIAZOLES; SUPPRESSOR; SIRTUINS;

D O I：

10.3390/molecules22081348

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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 mu M) was predicted using the CDOCKER program. The results of this research could provide informative guidance for further optimizing benzofuran derivatives as potent SIRT2 inhibitors.

引用

页数：12

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