Discovery of wrightiadione as a novel template for the TrkA kinase inhibitors

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Enzymatic kinase assays and docking simulation studies have shown that the natural product wrightiadione displays inhibitory activity toward TrkA and PLK3. In this study, the template of wrightiadione served as a starting point for Trk inhibitor development campaigns. Molecular simulation provided structural insights for the design of derivatives that were efficiently generated by our recently developed 3-step tandem synthetic approach, resulting in the discovery of compound 2h with biochemical potency at the single-digit micromolar level.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Issue Date
2015-11
Language
English
Article Type
Article
Keywords

ANTICANCER AGENTS; IDENTIFICATION; RECEPTOR; POTENT; DERIVATIVES; COVERAGE; DESIGN; KINOME; CANCER; DRUGS

Citation

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.25, no.22, pp.5186 - 5189

ISSN
0960-894X
DOI
10.1016/j.bmcl.2015.09.070
URI
http://hdl.handle.net/10203/207493
Appears in Collection
CH-Journal Papers(저널논문)
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