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

Virginie Bellet; Laure Lichon; Dominique Arama; Audrey Gallud; Vincent Lisowski; Ludovic Maillard; Marcel Garcia; Jean Martinez; Nicolas Masurier

doi:10.1016/j.ejmech.2016.11.023

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

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

Virginie Bellet, Laure Lichon, Dominique Arama, Audrey Gallud, Vincent Lisowski, Ludovic Maillard, Marcel Garcia, Jean Martinez et Nicolas Masurier

European Journal of Medicinal Chemistry, Vol.125, pp.1225-1234

2017

DOI: https://doi.org/10.1016/j.ejmech.2016.11.023

Résumé

Imidazo[1-2-a]pyridine

Polyfused heterocycles

Diazepinones

Antitumor activity

Melanoma

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 μM concentration, and high selectivity against the melanoma cell line MDA-MB-435.

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Titre: Imidazopyridine-fused [1,3]-diazepinones part 2: Structure-activity relationships and antiproliferative activity against melanoma cells
Créateurs - sans rôle: Virginie Bellet - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Laure Lichon - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Dominique Arama - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Audrey Gallud - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Vincent Lisowski - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Ludovic Maillard - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Marcel Garcia - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Jean Martinez - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Nicolas Masurier - Université de Montpellier, Institut des Biomolécules Max Mousseron - IBMM
Détails de publication: European Journal of Medicinal Chemistry, Vol.125, pp.1225-1234
Identifiants: 99150582409311
Unité académique: Institut des Biomolécules Max Mousseron - IBMM
Langue: English
Type de ressource: Journal article
Champs locaux: hal-03116585