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

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Title
Discovery of wrightiadione as a novel template for the TrkA kinase inhibitors
Author(s)
Yujeong Jeong; Sang Min Lim; Sungwoo Hong
Publication Date
2015-11
Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.25, no.22, pp.5186 - 5189
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Abstract
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. © 2015 Elsevier Ltd. All rights reserved
URI
https://pr.ibs.re.kr/handle/8788114/1844
ISSN
0960-894X
Appears in Collections:
Center for Catalytic Hydrocarbon Functionalizations(분자활성 촉매반응 연구단) > Journal Papers (저널논문)
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