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

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Tatum PR,Sawada H,Ota Y,Itoh Y,Zhan P,Ieda N,Nakagawa H,Miyata N,Suzuki T

doi

10.1016/j.bmcl.2014.03.026

subject

Has Abstract

pub_date

2014-04-15 00:00:00

pages

1871-4

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00242-X

journal_volume

24

pub_type

杂志文章

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