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

Authors: Altmann E.; Widler L.; Missbach M.

Source: Mini Reviews in Medicinal Chemistry, Volume 2, Number 3, June 2002 , pp. 201-208(8)

Publisher: Bentham Science Publishers

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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

Language: English

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1389557023406188

Publication date: 2002-06-01

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