Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties

…, AL Larroque, J McNamee, BJ Jean-Claude

Index: Rachid, Zakaria; Katsoulas, Athanasia; Williams, Christopher; Larroque, Anne-Laure; McNamee, James; Jean-Claude, Bertrand J. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 15 p. 4248 - 4253

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Citation Number: 10

Abstract

Steps toward the identification of combi-molecules with strong abl tyrosine kinase (TK) inhibitory property and significant DNA damaging potential are described. The optimized combi-molecule 13a was shown to induce approximately twofold stronger abl TK inhibitory activity than Gleevec™ and high levels of DNA damage in chronic myelogenous leukemic cells.