Synthesis and identification of GZD856 as an orally bioavailable Bcr-AblT315I inhibitor overcoming acquired imatinib resistance

Synthesis and identification of GZD856 as an orally bioavailable Bcr-AblT315I inhibitor overcoming acquired imatinib resistance

Bcr-AblT315I induced drug resistance remains a major challenge to chronic myelogenous leukemia (CML) treatment. Herein, we reported GZD856 as a novel orally bioavailable Bcr-AblT315I inhibitor, which strongly suppressed the kinase activities of both native Bcr-Abl and the T315I mutant with IC50 valu...

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Bibliographic Details
Main Authors: Xiaoyun Lu, Zhang Zhang, Xiaomei Ren, Deping Wang, Ke Ding
Format: Article
Language:English
Published: Taylor & Francis Group 2017-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
Bcr-Abl
chronic myelogenous leukemia
imatinib clinical resistance
scaffold hopping
T315I mutant
Online Access:http://dx.doi.org/10.1080/14756366.2016.1250757

Internet

http://dx.doi.org/10.1080/14756366.2016.1250757

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