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Bioorg Med Chem. 2012 Feb 15;20(4):1475-81. doi: 10.1016/j.bmc.2011.12.054. Epub 2012 Jan 11.

Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors.

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1
Department 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.

PMID:
22285028
DOI:
10.1016/j.bmc.2011.12.054
[Indexed for MEDLINE]
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