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

Qianyi Chen, Vashti C. Bryant, Hernando Lopez, David L. Kelly, Xu Luo, Amarnath Natarajan

Research output: Contribution to journalArticle

25 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)1929-1932
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number7
DOIs
StatePublished - Apr 1 2011

Keywords

  • Antiproliferative
  • Mcl-1 dependent apoptosis
  • Quinoxaline urea

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of '2,3-Substituted quinoxalin-6-amine analogs as antiproliferatives: A structure-activity relationship study'. Together they form a unique fingerprint.

  • Cite this