Discovery of a Candidate Containing an (S)-3,3-Difluoro-1-(4-methylpiperazin-1-yl)-2,3-dihydro-1H-inden Scaffold as a Highly Potent Pan-Inhibitor of the BCR-ABL Kinase Including the T315I-Resistant Mutant for the Treatment of Chronic Myeloid Leukemia.
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DOI: 10.1021/acs.jmedchem.1c00082
Abstract: BCR-ABL kinase inhibition is an effective strategy for the treatment of chronic myeloid leukemia (CML). Herein, we report compound 3a-P1, bearing a difluoro-indene scaffold, as a novel potent pan-inhibitor against BCR-ABL mutants, including the most… read more here.
Keywords: bcr; abl kinase; bcr abl; t315i ... See more keywords
Abstract 1980: S116836 overcomes BCR-ABL T315I mutation mediated imatinib resistance in chronic myeloid leukemia
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DOI: 10.1158/1538-7445.am2018-1980
Abstract: Chronic Myeloid Leukemia (CML) is largely caused by the Philadelphia (Ph) chromosome carrying the Break point Cluster Region-Abelson (BCR-ABL) oncogene. Imatinib is a BCR-ABL-targeted therapy and considered the standard of care in CML management. Resistance… read more here.
Keywords: bcr abl; resistance; t315i; baf3 ... See more keywords
The Potential Inhibitors in Traditional Chinese Medicine for BCR-ABL T315I Mutation of Chronic Myelogenous Leukemia
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DOI: 10.4172/2161-0444.1000496
Abstract: Chronic Myelogenous Leukemia (CML) is a myeloproliferative disorder characterized by the appearance of abnormal proliferation of white blood cells in the Philadelphia chromosome. Current drugs target ABL kinase may have resistance or have risks of… read more here.
Keywords: medicine; potential inhibitors; chronic myelogenous; myelogenous leukemia ... See more keywords