Abstract
Indole-3-carbinol is a natural product which has been shown to reduce the incidence of spontaneous and carcinogen-induced mammary tumours in animals. Eighteen unsymmetrical methylene derivatives of indoles were prepared by reaction of Mannich bases of 7-hydroxycoumarins with substituted indoles in acetic or propionic anhydride. The synthesised molecules were tested in vitro against the MCF7 and MDA-MB-231 breast cancer cell lines by MTT and cell count assays. Results from 16 tested compounds showed that 60% of them exerted some effects against the MDA-MB-231 compared to about 30% towards the MCF7. Among all, the 3-(7′-acetoxy-4-methylcoumarin-8′-yl)methyl-2-methylindole resulted the most effective in both cell lines, compared to indole-3-carbinol. In conclusion, these preliminary results report that some of these compounds might be promising potential antiproliferative agents.
Original language | English |
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Pages (from-to) | 915-923 |
Number of pages | 9 |
Journal | European Journal of Medicinal Chemistry |
Volume | 36 |
Issue number | 11-12 |
DOIs | |
Publication status | Published - Dec 1 2001 |
Keywords
- Antiproliferative agents
- Coumarins
- Indole-3-carbinol
- Indoles
- Unsymmetrical methylene derivatives
ASJC Scopus subject areas
- Molecular Medicine
- Organic Chemistry
- Drug Discovery
- Pharmaceutical Science