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Bioorg Med Chem Lett. 2011 Apr 1;21(7):1929-32. doi: 10.1016/j.bmcl.2011.02.055. Epub 2011 Feb 17.

2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: a structure-activity relationship study.

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1
Eppley Institute for Cancer Research, University of Nebraska Medical Center, Omaha, NE 68198, United States.

Abstract

The quinoxaline core is considered a privileged scaffold as it is found in a variety of biologically relevant molecules. Here we report the synthesis of a quinoxalin-6-amine library, screening against a panel of cancer cell lines and a structure-activity relationship (SAR). This resulted in the identification of a bisfuranylquinoxalineurea analog (7c) that has low micromolar potency against the panel of cancer cell lines. We also show that cells treated with quinoxalineurea 7c results in caspase 3/7 activation, PARP cleavage and Mcl-1 dependent apoptosis.

PMID:
21376584
PMCID:
PMC3063321
DOI:
10.1016/j.bmcl.2011.02.055
[Indexed for MEDLINE]
Free PMC Article
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