3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: Design and development to a highly selective lead

被引：25

作者：

Soth, Michael ^{[1
]}

Abbot, Sarah ^{[1
]}

Abubakari, Allassan ^{[1
]}

Arora, Nidhi ^{[1
]}

Arzeno, Humberto ^{[1
]}

Billedeau, Roland ^{[1
]}

Dewdney, Nolan ^{[1
]}

Durkin, Kieran ^{[1
]}

Frauchiger, Sandra ^{[1
]}

Ghate, Manjiri ^{[1
]}

Goldstein, David M. ^{[1
]}

Hill, Ronald J. ^{[1
]}

Kuglstatter, Andreas ^{[1
]}

Li, Fujun ^{[1
]}

Loe, Brad ^{[1
]}

McCaleb, Kristen ^{[1
]}

McIntosh, Joel ^{[1
]}

Papp, Eva ^{[1
]}

Park, Jaehyeon ^{[1
]}

Stahl, Martin ^{[2
]}

Sung, Man-Ling ^{[1
]}

Suttman, Rebecca ^{[1
]}

Swinney, David C. ^{[1
]}

Weller, Paul ^{[1
]}

Wong, Brian ^{[1
]}

Zecic, Hasim ^{[1
]}

Gabriel, Tobias ^{[1
]}

机构：

[1] Roche Palo Alto, Palo Alto, CA 94304 USA

[2] F Hoffmann La Roche & Cie AG, Discovery Chem, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 11期

关键词：

p38; Kinase; Kinase inhibitor; P38 MAP KINASE; INCREMENTAL CONSTRUCTION; FORCE-FIELD; DISCOVERY; PAMAPIMOD; EFFICACY; PATHWAY;

D O I：

10.1016/j.bmcl.2011.03.098

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：3452 / 3456

页数：5

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