P3 SAR exploration of biphenyl carbamate based Legumain inhibitors

被引：11

作者：

Higgins, Catherine ^{[1
]}

Bouazzaoui, Samira ^{[1
]}

Gaddale, Kishore ^{[1
]}

D'Costa, Zenobia ^{[1
]}

Templeman, Amy ^{[1
]}

O'Rourke, Martin ^{[2
]}

Young, Andrew ^{[3
]}

Scott, Christopher ^{[1
,3
]}

Harrison, Tim ^{[1
,2
]}

Mullan, Paul ^{[1
]}

Williams, Rich ^{[1
]}

机构：

[1] Queens Univ Belfast, CCRCB Drug Discovery Grp, Ctr Canc Res & Cell Biol, Belfast BT9 7BL, Antrim, North Ireland

[2] Almac Discovery, Craigavon BT63 5QD, North Ireland

[3] Queens Univ Belfast, Sch Pharm, Belfast BT9 7BL, Antrim, North Ireland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 11期

关键词：

Legumain; Cancer; Cyano warhead; Protease inhibitor; ASPARAGINE ENDOPEPTIDASE; IDENTIFICATION;

D O I：

10.1016/j.bmcl.2014.04.002

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This Letter describes the further development and SAR exploration of a novel series of Legumain inhibitors. Based upon a previously identified Legumain inhibitor from our group, we explored the SAR of the carbamate phenyl ring system to probe the P3 pocket of the enzyme. This led to the identification of a sub-nanomolar inhibitor of Legumain. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：2521 / 2524

页数：4

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