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Molecules 2017, 22(8), 1348; doi:10.3390/molecules22081348

Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors

1
College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China
2
Institute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China
3
Institute of MateriaMedica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
*
Authors to whom correspondence should be addressed.
Received: 10 July 2017 / Revised: 6 August 2017 / Accepted: 8 August 2017 / Published: 14 August 2017
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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. View Full-Text
Keywords: benzofuran; sulfoxide; sulfone; selective SIRT2 inhibitor benzofuran; sulfoxide; sulfone; selective SIRT2 inhibitor
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Zhou, Y.; Cui, H.; Yu, X.; Peng, T.; Wang, G.; Wen, X.; Sun, Y.; Liu, S.; Zhang, S.; Hu, L.; Wang, L. Synthesis and Evaluation of Novel Benzofuran Derivatives as Selective SIRT2 Inhibitors. Molecules 2017, 22, 1348.

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