title: 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: University of Calabria, Department of Pharmaceutical Sciences, 87036 Arcavacata di Rende (CS), Italy.
authors: Maria Stefania
authors: MS
authors: Sinicropi
authors: Anna
authors: A
authors: Caruso
authors: Filomena
authors: F
authors: Conforti
authors: Mariangela
authors: M
authors: Marrelli
authors: Hussein
authors: H
authors: El Kashef
authors: Jean-charles
authors: JC
authors: Lancelot
authors: Sylvain
authors: S
authors: Rault
authors: Giancarlo A
authors: GA
authors: Statti
authors: Francesco
authors: F
authors: Menichini
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D051379:Mice; D015394:Molecular Structure; D009569:Nitric Oxide / Q000037:antagonists & inhibitors*; D011714:Pyrans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D011714:Pyrans; D009569:Nitric Oxide