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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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

Author(s): Eva Altmann, Leo Widler and Martin Missbach

Volume 2, Issue 3, 2002

Page: [201 - 208] Pages: 8

DOI: 10.2174/1389557023406188

Price: $65

Abstract

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.

Keywords: tyrosine kinase inhibitor, c-src inhibitor

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