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

…, W Breitenstein, J Brüggen, SW Cowan-Jacob…

Index: Manley, Paul W.; Breitenstein, Werner; Brueggen, Josef; Cowan-Jacob, Sandra W.; Furet, Pascal; Mestan, Juergen; Meyer, Thomas Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 23 p. 5793 - 5797

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Citation Number: 65

Abstract

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 IC50 value of 56nM. Although this activity was not translated ...