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ID: ALA3627674
Journal: Bioorg Med Chem Lett
Title: Discovery of wrightiadione as a novel template for the TrkA kinase inhibitors.
Authors: Jeong Y, Lim SM, Hong S.
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.
CiteXplore: 26442778