Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596264 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
Based on screening hit 1, a series of tricyclic quinoxalinones have been designed and evaluated for inhibition of PARP-1. Substitutions at the 7- and 8-positions of the quinoxalinone ring led to a number of compounds with good enzymatic and cellular potency. The tricyclic quinoxalinone class is sensitive to modifications of both the amine substituent and the tricyclic core. The synthesis and structure-activity relationship studies are presented.
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Authors
Julie Miyashiro, Keith W. Woods, Chang H. Park, Xuesong Liu, Yan Shi, Eric F. Johnson, Jennifer J. Bouska, Amanda M. Olson, Yan Luo, Elizabeth H. Fry, Vincent L. Giranda, Thomas D. Penning,