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Synthesis and SAR of Novel Tricyclic Quinoxalinone Inhibitors of Poly(ADP-ribose)polymerase-1 (PARP-1)

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Specialty Biochemistry
Date 2009 Jun 26
PMID 19553114
Citations 23
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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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