Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors

被引：69

作者：

Nærum, L ^{[1
]}

Norskov-Lauritsen, L ^{[1
]}

Olesen, PH ^{[1
]}

机构：

[1] Novo Nordisk AS, Med Chem Res, DK-2760 Molov, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(02)00169-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Using a virtual screening strategy based on a methodology derived from the CATS molecular descriptor, a novel compound class with inhibitory activity against the GSK-3 enzyme was identified through scaffold hopping. These compounds were readily synthesized, either by solid-phase or solution-phase chemistry. Compounds with inhibitory activity below 1 muM were identified. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1525 / 1528

页数：4

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