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Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.

Manley, Paul W., Breitenstein, Werner, Brueggen, Josef, Cowan-Jacob, Sandra W, Furet, Pascal, Mestan, Juergen and Meyer, Thomas (2004) Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases. Bioorganic & Medicinal Chemistry Letters, 14 (23). pp. 5793-5797. ISSN 0960-894X


The constitutively active Abl kinase activity of the Bcr-Abl oncoprotein is causative for chronic myelogenous leukemia. Urea derivatives, structurally related to the therapeutic agent STI571, have been identified, which potently inhibit the tyrosine kinase activity of recombinant Abl. In particular a dimethylamino-aniline derivative (18) inhibited c-Abl transphosphorylation with an IC(50) value of 56 nM. Although this activity was not translated into cellular activity against the constitutively activated oncogenic Bcr-Abl, a number of compounds from this series potently inhibited cellular PDGFR autophosphorylation. It was also possible to differentiate between c-Abl and PDGFR kinase inhibition, with compound 22 being selective towards Abl and 23 selective for PDGFR.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Gleevec; Tyrosine kinase
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Date Deposited: 14 Dec 2009 13:55
Last Modified: 31 Jan 2013 01:08


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