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Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors

Literature Life Science

Chk1 and Chk2 inhibition effect of analogs of the marine sponge metabolite using a HTRF serine/threonine KinEASE assay

Abstract

Natural products have been the subject of interest for drug discovery and as tools for understanding the underlying cellular pathways in various diseases. We present herein the synthesis and evaluation of new analogs of the marine sponge metabolite, debromohymenialdisine, as checkpoint kinase 2 (Chk2) inhibitors. We illustrate herein that slight modifications to the natural product scaffold can induce strong selectivity for Chk2 over Chk1. These Chk2 inhibitors can serve as drug templates or molecular tools to gain insight in Chk2 mediated radioprotectio

Details

Bioorg Med Chem. 2012;20(4):1475-81.

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