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.
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页码：201 / 208
页数：8
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