4.7 Article

Imidazopyridine-fused [1,3]-diazepinones part 2: Structure-activity relationships and antiproliferative activity against melanoma cells

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 125, Issue -, Pages 1225-1234

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.11.023

Keywords

Imidazo[1,2-a]pyridine; Polyfused heterocycles; Diazepinones; Antitumor activity; Melanoma

Funding

  1. Ligue Nationale contre le Cancer (Comite de l'Herault)

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We recently described a pyrido-imidazodiazepinone derivative which could be a promising hit compound for the development of new drugs acting against melanoma cells. In this study, a series of 28 novel pyrido-imidazodiazepinones were synthesized and screened for their in vitro cytotoxic activities against the melanoma MDA-MB-435 cell line. Among the derivatives, seven of them showed 50% growth inhibitory activity at 1 mu M concentration, and high selectivity against the melanoma cell line MDA-MB-435. (C) 2016 Elsevier Masson SAS. All rights reserved.

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