The development of novel 1,2-dihydro-pyrimido[4,5-c]pyridazine based inhibitors of lymphocyte specific kinase (Lck)

被引：23

作者：

Sabat, Mark ^{[1
]}

VanRens, John C. ^{[1
]}

Brugel, Todd A. ^{[1
]}

Maier, Jennifer ^{[1
]}

Laufersweiler, Matthew J. ^{[1
]}

Golebiowski, Adam ^{[1
]}

De, Biswanath ^{[1
]}

Easwaran, ViJayasurian ^{[1
]}

Hsieh, Lily C. ^{[1
]}

Rosegen, Jeff ^{[1
]}

Berberich, Steve ^{[1
]}

Suchanek, Eric ^{[1
]}

Janusz, Michael J. ^{[1
]}

机构：

[1] Procter & Gamble Pharmaceut, Hlth Care Res Ctr, Mason, OH 45040 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 16期

关键词：

Lck; lymphocyte specific kinase; T-cell; pyridazines;

D O I：

10.1016/j.bmcl.2006.05.072

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This communication details the synthesis, biological activity, and proposed binding mode of a novel class of tri-cyclic derivatives of 1,2-dihydro-pyrimido[4,5-c]pyridazines 1 and 2. The most potent analogs disclosed showed low nanomolar activity for the inhibition of Lck kinase. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：4257 / 4261

页数：5

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