2. Academic Validation
  3. Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties

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

  • Bioorg Med Chem Lett. 2007 Aug 1;17(15):4248-53. doi: 10.1016/j.bmcl.2007.05.067.
Zakaria Rachid 1,  Athanasia Katsoulas,  Christopher Williams,  Anne-Laure Larroque,  James McNamee,  Bertrand J Jean-Claude
Affiliations

Affiliation

  • 1 Cancer Drug Research Laboratory, Division of Medical Oncology, Department of Medicine, McGill University/Royal Victoria Hospital, 687 Pine Avenue West Rm. M-719, Montreal, Que., Canada H3A 1A1.
PMID: 17572088 DOI: 10.1016/j.bmcl.2007.05.067
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.

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