Synthesis,inhibition of NO production and antiproliferative activities of some indole derivatives |
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| Authors: | Maria Stefania Sinicropi Anna Caruso Mariangela Marrelli Hussein El Kashef Jean-charles Lancelot |
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| Institution: | 1. University of Calabria, Department of Pharmaceutical Sciences, 87036 Arcavacata di Rende (CS), Italy;2. Université de Caen Basse-Normandie, U.F.R. des Sciences Pharmaceutiques, Centre d’Etudes et de Recherche sur le Médicament de Normandie, UPRES EA-3915 FR CNRS INC3M, 5, rue Vaubénard, 14032 Caen Cedex, France |
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| Abstract: | The synthesis and the biological evaluation of pyrano3,2-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 (IC50?=?1.1?μM and IC50?=?2.3 μM respectively). Compound 5a was the most active against melanotic melanoma (IC50?=?11.8?μM) while the other compounds exhibited weak cytotoxicity with IC50 values >50?μM on all cell lines. |
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| Keywords: | Pyrano[3 2-e]indoles indole derivatives von Pechmann reaction coumarin derivatives inhibition of NO production antiproliferative effect |
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