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

Autor: Rachid Z; 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., Katsoulas A, Williams C, Larroque AL, McNamee J, Jean-Claude BJ
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Aug 01; Vol. 17 (15), pp. 4248-53. Date of Electronic Publication: 2007 May 24.
DOI: 10.1016/j.bmcl.2007.05.067
Abstrakt: 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.
Databáze: MEDLINE