Synthesis, inhibition of NO production and antiproliferative activities of some indole derivatives.

Abstract

The synthesis and the biological evaluation of pyrano[3,2-e]indoles and their reaction intermediates are described. The compounds prepared were evaluated for their inhibition of NO production, antioxidant activity and also for their ability to inhibit in vitro the growth of four human tumor cell lines: large lung carcinoma (COR-L23), alveolar basal epithelial carcinoma (A549), amelanotic melanoma (C32) and melanoma (A375). The two reaction intermediates, 5a and 5b, showed the highest inhibition of NO production in murine monocytic macrophage (IC(50) = 1.1 microM and IC(50) = 2.3 microM respectively). Compound 5a was the most active against melanotic melanoma (IC(50) = 11.8 microM) while the other compounds exhibited weak cytotoxicity with IC(50) values >50 microM on all cell lines.

• Authors: Maria Stefania Sinicropi, Anna Caruso, Filomena Conforti, Mariangela Marrelli, Hussein El Kashef, Jean-charles Lancelot, Sylvain Rault, Giancarlo A Statti, Francesco Menichini
• Journal: Journal of enzyme inhibition and medicinal chemistry (J Enzyme Inhib Med Chem) Vol. 24 Issue 5 Pg. 1148-53 (Oct 2009) ISSN: 1475-6374 [Electronic] England
• PMID: 19555184 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Indoles
• Pyrans
• Nitric Oxide

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Humans
• Indoles (chemical synthesis, chemistry, pharmacology)
• Inhibitory Concentration 50
• Mice
• Molecular Structure
• Nitric Oxide (antagonists & inhibitors)
• Pyrans (chemical synthesis, chemistry, pharmacology)