Anticancer activities of novel chalcone and bis-chalcone derivatives

Aneta Modzelewska, Catherine Pettit, Geetha Achanta, Nancy E. Davidson, Peng Huang, Saeed R. Khan

Research output: Contribution to journalArticlepeer-review

Abstract

A series of novel chalcones and bis-chalcones containing boronic acid moieties has been synthesized and evaluated for antitumor activity against the human breast cancer MDA-MB-231 (estrogen receptor-negative) and MCF7 (estrogen receptor-positive) cell lines and against two normal breast epithelial cell lines, MCF-10A and MCF-12A. These molecules inhibited the growth of the human breast cancer cell lines at low micromolar to nanomolar concentrations, with five of them (1-4, 9) showing preferential inhibition of the human breast cancer cell lines. Furthermore, bis-chalcone 8 exhibited a more potent inhibition of colon cancer cells expressing wild-type p53 than of an isogenic cell line that was p53-null.

Original languageEnglish (US)
Pages (from-to)3491-3495
Number of pages5
JournalBioorganic and Medicinal Chemistry
Volume14
Issue number10
DOIs
StatePublished - May 15 2006

Keywords

  • Anticancer
  • Bis-chalcone
  • Chalcone
  • Claisen-Schmidt reaction

ASJC Scopus subject areas

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

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