Overcoming resistance: In an effort to optimize our previously identified dual Src/Abl hits, a new series of 1,3,4-thiadiazoles and 1,3-thiazoles were designed and synthesized, paying particular attention to the reduction of their lipophilicity and to the improvement of the affinity towards the drug-resistant T315I mutant. Compound 5 was identified as a promising allosteric inhibitor of the T315I mutant.
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|Titolo:||Design and synthesis of Thiadiazoles and Thiazoles targeting the Bcr-Abl T315I mutant: from docking false positives to ATP-noncompetitive inhibitors|
|Citazione:||Botta, M., Crespan, E., Falchi, F., Bernardo, V., Zanoli, S., Manetti, F., et al. (2010). Design and synthesis of Thiadiazoles and Thiazoles targeting the Bcr-Abl T315I mutant: from docking false positives to ATP-noncompetitive inhibitors. CHEMMEDCHEM, 5, 1226-1231.|
|Appare nelle tipologie:||1.1 Articolo in rivista|