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Title: Rapid synthesis of Abelson tyrosine kinase inhibitors using click chemistry
Authors: Kalesh, K.A.
Liu, K.
Yao, S.Q. 
Issue Date: 2009
Citation: Kalesh, K.A., Liu, K., Yao, S.Q. (2009). Rapid synthesis of Abelson tyrosine kinase inhibitors using click chemistry. Organic and Biomolecular Chemistry 7 (24) : 5129-5136. ScholarBank@NUS Repository.
Abstract: Protein kinases catalyze the phosphorylation of serine, threonine, tyrosine and histidine residues in proteins. Aberrant regulation of kinase activity has been implicated in many diseases including cancer. Thus development of new strategies for kinase inhibitor design remains an active area of research with direct relevance to drug development. Abelson (Abl) tyrosine kinase is one of the Src-family of tyrosine kinases and is directly implicated in Chronic Myelogenous Leukemia (CML). In this article, we have, for the first time, developed an efficient method for the construction of small molecule-based bisubstrate inhibitors of Abl kinase using click chemistry. Subsequent biochemical screenings revealed a set of moderately potent inhibitors, a few of which have comparable potency to Imatinib (an FDA-approved drug for treatment of chronic myeloid leukemia) against Abl. © 2009 The Royal Society of Chemistry.
Source Title: Organic and Biomolecular Chemistry
ISSN: 14770520
DOI: 10.1039/b913333j
Appears in Collections:Staff Publications

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