Identification of novel SIRT2-selective inhibitors using a click chemistry approach

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:24

Article

Tatum, Prima R.¹  Sawada, Hideyuki²  Ota, Yosuke²  Itoh, Yukihiro²  Zhan, Peng²  Ieda, Naoya¹  Nakagawa, Hidehiko¹  Miyata, Naoki¹  Suzuki, Takayoshi² 

[1] Nagoya City Univ, Grad Sch Pharmaceut Sci, Mizuho Ku, Nagoya, Aichi 4678603, Japan

[2] Kyoto Prefectural Univ Med, Grad Sch Med Sci, Kita Ku, Kyoto 6038334, Japan

关键词: Sirtuin;    Histone deacetylase;    Inhibitor;    Isozyme selectivity;   

DOI  :  10.1016/j.bmcl.2014.03.026

来源: Elsevier

【 摘 要 】

A series of 114 SIRT inhibitor candidates was assembled using 'click chemistry', by reacting two alkynes bearing 2-anilinobenzamide pharmacophore with 57 azide building blocks in the presence of Cu( I) catalyst. Screening identified two SIRT2-selective inhibitors, which were more SIRT2-selective than AGK2, a known SIRT2 inhibitor. These findings will be useful for further development of SIRT2-selective inhibitors. (C) 2014 Elsevier Ltd. All rights reserved.

【 授权许可】

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