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.
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 [10.1002/cmdc.201000066].
Design and synthesis of Thiadiazoles and Thiazoles targeting the Bcr-Abl T315I mutant: from docking false positives to ATP-noncompetitive inhibitors
BOTTA, MAURIZIO;MANETTI, FABRIZIO;
2010-01-01
Abstract
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.File | Dimensione | Formato | |
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https://hdl.handle.net/11365/21146
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