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

Year: 2009

Type: article

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.

Source: Journal of Enzyme Inhibition and Medicinal Chemistry

DOI: 10.1080/14756360802693890

Authors: Maria Stefania Sinicropi, Anna Caruso, Filomena Conforti, Mariangela Marrelli, Hussein El Kashef, Jean-charles Lancelot, Sylvain Rault, Giancarlo A. Statti, Francesco Menichini

Institutions: University of Calabria, Centre National de la Recherche Scientifique, Centre d'Etudes et de Recherche sur le Médicament de Normandie, Université de Caen Normandie

Language: English

Topic: Heterocyclic Compound Synthesis and Bioactivity

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: bronze

OpenAlex ID: W2029319917

FWCI: 0.604

Cites: 30

Cited by: 42

Related to: 10