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 language | English (US) |
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Pages (from-to) | 3491-3495 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry |
Volume | 14 |
Issue number | 10 |
DOIs | |
State | Published - May 15 2006 |
Externally published | Yes |
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