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Published on: January 22, 2019
Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors
Rahman Shah Zaib Saleem1, Theresa A Lansdell, Jetze J Tepe
1Department of Chemistry, Michigan State University, East Lansing, MI 48824, USA.
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 radioprotection.
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