European Journal of Medicinal Chemistry 2010-03-01

5-Substituted [1]pyrindine derivatives with antiproliferative activity.

Stéphanie Kolb, Mary-Lorène Goddard, Ali Loukaci, Odile Mondésert, Bernard Ducommun, Emmanuelle Braud, Christiane Garbay

Index: Eur. J. Med. Chem. 45 , 896-901, (2010)

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Abstract

We report herein the synthesis of 5-substituted [1]pyrindine derivatives and the evaluation of their antiproliferative properties on HeLa cells, a cervical carcinoma tumor cell line, and on the melanoma A2058 cell line. The most efficient compounds display cytotoxicity against tumor cells in the micromolar range but have interestingly no effect against the normal human fibroblasts CRL-2796. Generally, these pyrindines are active on both tumor cell lines. Compounds bearing large substituents with structural rigidity at position 5 such as phenyl-furyl show no inhibition of cell growth.Copyright (c) 2009 Elsevier Masson SAS. All rights reserved.