Identification of benzofuran-3-yl (phenyl) methanones as novel SIRT1 inhibitors: binding mode, inhibitory mechanism and biological action

J Wu, Y Li, K Chen, H Jiang, MH Xu, D Liu

文献索引：Wu, Jiahui; Li, Yi; Chen, Kaixian; Jiang, Hualiang; Xu, Ming-Hua; Liu, Dongxiang European Journal of Medicinal Chemistry, 2013 , vol. 60, p. 441 - 450

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被引用次数: 6

摘要

SIRT1 is a NAD+-dependent deacetylase. Here we described new SIRT1 inhibitors with the scaffold of benzofuran-3-yl (phenyl) methanone. The inhibitors were predicted to bind in C- pocket of SIRT1, forming hydrophobic interactions with Phe273, Phe312 and Ile347. Introducing hydroxyl to meta position of phenyl may form H-bond with Asn346. Indeed,(2, 5- dihydroxyphenyl)(5-hydroxy-1-benzofuran-3-yl) methanone (16), an analogue with ...