Synthesis, inhibition of NO production and antiproliferative activities of some indole derivatives.
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.
Sinicropi
Maria Stefania
MS
University of Calabria, Department of Pharmaceutical Sciences, 87036 Arcavacata di Rende (CS), Italy.
Caruso
Anna
A
Conforti
Filomena
F
Marrelli
Mariangela
M
El Kashef
Hussein
H
Lancelot
Jean-charles
JC
Rault
Sylvain
S
Statti
Giancarlo A
GA
Menichini
Francesco
F
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
D000970:Antineoplastic Agents; D007211:Indoles; D011714:Pyrans; D009569:Nitric Oxide