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
Mini-Reviews in Medicinal Chemistry
Title: N7-Substituted-5-aryl-pyrrolo[2,3-d]pyrimidines Represent a Versatile Class of Potent Inhibitors of the Tyrosine Kinase c-Src
Volume: 2 Issue: 3
Author(s): Eva Altmann, Leo Widler and Martin Missbach
Affiliation:
Keywords: tyrosine kinase inhibitor, c-src inhibitor
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.
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Cite this article as:
Altmann Eva, Widler Leo and Missbach Martin, N7-Substituted-5-aryl-pyrrolo[2,3-d]pyrimidines Represent a Versatile Class of Potent Inhibitors of the Tyrosine Kinase c-Src, Mini-Reviews in Medicinal Chemistry 2002; 2 (3) . https://dx.doi.org/10.2174/1389557023406188
DOI https://dx.doi.org/10.2174/1389557023406188 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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