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