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

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Rachid Z, Katsoulas A, Williams C, Larroque AL, McNamee J, Jean-Claude BJ

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. Epub 2007 May 24.

PubMed ID

17572088 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Imatinib	Tyrosine-protein kinase ABL1	IC 50 (nM)	40	N/A	N/A	Details