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 journalArticle

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

Fingerprint

Chalcone
Cells
Derivatives
Cell Line
Chalcones
Breast Neoplasms
Estrogen Receptors
Boronic Acids
Human Activities
Colonic Neoplasms
Breast
Epithelial Cells
Molecules
Growth

Keywords

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

ASJC Scopus subject areas

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

Cite this

Modzelewska, A., Pettit, C., Achanta, G., Davidson, N. E., Huang, P., & Khan, S. R. (2006). Anticancer activities of novel chalcone and bis-chalcone derivatives. Bioorganic and Medicinal Chemistry, 14(10), 3491-3495. https://doi.org/10.1016/j.bmc.2006.01.003

Anticancer activities of novel chalcone and bis-chalcone derivatives. / Modzelewska, Aneta; Pettit, Catherine; Achanta, Geetha; Davidson, Nancy E.; Huang, Peng; Khan, Saeed R.

In: Bioorganic and Medicinal Chemistry, Vol. 14, No. 10, 15.05.2006, p. 3491-3495.

Research output: Contribution to journalArticle

Modzelewska, A, Pettit, C, Achanta, G, Davidson, NE, Huang, P & Khan, SR 2006, 'Anticancer activities of novel chalcone and bis-chalcone derivatives', Bioorganic and Medicinal Chemistry, vol. 14, no. 10, pp. 3491-3495. https://doi.org/10.1016/j.bmc.2006.01.003
Modzelewska A, Pettit C, Achanta G, Davidson NE, Huang P, Khan SR. Anticancer activities of novel chalcone and bis-chalcone derivatives. Bioorganic and Medicinal Chemistry. 2006 May 15;14(10):3491-3495. https://doi.org/10.1016/j.bmc.2006.01.003
Modzelewska, Aneta ; Pettit, Catherine ; Achanta, Geetha ; Davidson, Nancy E. ; Huang, Peng ; Khan, Saeed R. / Anticancer activities of novel chalcone and bis-chalcone derivatives. In: Bioorganic and Medicinal Chemistry. 2006 ; Vol. 14, No. 10. pp. 3491-3495.
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