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

European journal of medicinal chemistry (2009-12-09)
Stéphanie Kolb, Mary-Lorène Goddard, Ali Loukaci, Odile Mondésert, Bernard Ducommun, Emmanuelle Braud, Christiane Garbay
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Menadione, crystalline
Supelco
Menadione (K3), analytical standard
Sigma-Aldrich
Menadione, meets USP testing specifications
A2058, 91100402

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