Aminopyridinecarboxamide-based inhibitors: Structure-activity relationship

被引：5

作者：

Bonafoux, Dominique F. ^{[1
]}

Bonar, Sheri L. ^{[2
]}

Clare, Michael ^{[1
]}

Donnelly, Ann M. ^{[2
]}

Glaenzer, Jeanette L. ^{[1
]}

Guzova, Julia A. ^{[2
]}

Huang, He ^{[1
]}

Kishore, Nandidni N. ^{[2
]}

Koszyk, Francis J. ^{[1
]}

Lennon, Patrick J. ^{[1
]}

Libby, Adam ^{[1
]}

Mathialagan, Sumathy ^{[2
]}

Oburn, David S. ^{[1
]}

Rouw, Sharon A. ^{[2
]}

Sommers, Cynthia D. ^{[2
]}

Tripp, Catherine S. ^{[2
]}

Vanella, Lori J. ^{[2
]}

Weier, Richard ^{[1
]}

Wolfson, Serge G. ^{[1
]}

Huang, Horng-Chih ^{[1
]}

机构：

[1] Pfizer Inc, Dept Med Chem, St Louis, MO 63017 USA

[2] Pfizer Inc, Dept Biol, St Louis, MO 63017 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 01期

关键词：

IKK2; NFkB; Inhibitor; NF-KAPPA-B; IKK-2; INHIBITOR; DISCOVERY;

D O I：

10.1016/j.bmc.2009.10.040

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Series of aminopyridinecarboxamide-based inhibitors were synthesized and tested against human recombinant IKK-2 and in IL-1 beta stimulated synovial. broblasts. The 2-amino-5-chloropyridine-4-carboxamides were identified as the most potent inhibitors with improved cellular activity. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：403 / 414

页数：12

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