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

Basic Information

ID: ALA1759840

Journal: Bioorg Med Chem Lett

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

Authors: Chen Q, Bryant VC, Lopez H, Kelly DL, Luo X, Natarajan A.

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.

CiteXplore: 21376584

DOI: 10.1016/j.bmcl.2011.02.055

Patent ID: