3-Aryl β-carbolin-1-ones as a new class of potent inhibitors of tumor cell proliferation: Synthesis and biological evaluation

Shaozhong Wang, Yanmei Dong, Xinyan Wang, Xiaoyi Hu, Jun O. Liu, Yuefei Hu

Research output: Contribution to journalArticle

Abstract

A novel three-step synthesis of 3-aryl β-carbolin-1-ones from non-indole starting materials has been developed. The two nitrogen atoms in β-carbolin-1-one were introduced efficiently by Michael addition of ethyl acetamidocyanoacetate to chalcone. The desired pyridone and indole rings were assembled by an intramolecular ketone-nitrile annulation mediated by aqueous HCl-HOAc and a Cu(i)-catalyzed intramolecular N-arylation of the amide, respectively. The target compounds were found to possess significant activity against tumor cell proliferaton.

Original languageEnglish (US)
Pages (from-to)911-916
Number of pages6
JournalOrganic and Biomolecular Chemistry
Volume3
Issue number5
DOIs
StatePublished - Mar 7 2005

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of '3-Aryl β-carbolin-1-ones as a new class of potent inhibitors of tumor cell proliferation: Synthesis and biological evaluation'. Together they form a unique fingerprint.

  • Cite this