N7-Substituted-5-aryl-pyrrolo[2,3-d]pyrimidines Represent a Versatile Class of Potent Inhibitors of the Tyrosine Kinase c-Src

被引：17

作者：

Altmann, Eva ^{[1
]}

Widler, Leo ^{[1
]}

Missbach, Martin ^{[1
]}

机构：

[1] Novartis Pharma AG, Therapeut Area Arthrit & Bone Metab, CH-4002 Basel, Switzerland

来源：

MINI-REVIEWS IN MEDICINAL CHEMISTRY | 2002年 / 2卷 / 03期

关键词：

D O I：

10.2174/1389557023406188

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Aryl-pyrrolo[2,3-d]pyrimidines incorporating different N7-substituents have been prepared and evaluated for their inhibitory potency towards the tyrosine kinase c-Src. Optimization of these compounds resulted in highly potent c-Src inhibitors, some (e. g. 4g, 6g, 7h, 8l) with excellent specificity towards other receptor and nonreceptor tyrosine kinases. In addition compounds 4g, 5b and 5c are characterized by a good pharmacokinetic profile.

引用

页码：201 / 208

页数：8

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