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

Journal article

Peer reviewed

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 and Nicolas Masurier

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

01/2017

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

PMID: 27871038

Abstract

Antitumor activity

Diazepinones

Imidazo[1

2-a]pyridine

Melanoma

Polyfused heterocycles

Antineoplastic Agents

Azepines

Cell Line, Tumor

Cell Proliferation

Drug Screening Assays, Antitumor

Humans

Pyridines

Structure-Activity Relationship

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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Title: Imidazopyridine-fused [1,3]-diazepinones part 2: Structure-activity relationships and antiproliferative activity against melanoma cells
Creators - without role: 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
Publication Details: European Journal of Medicinal Chemistry, Vol.125, pp.1225-1234
Identifiers: 9947052909311
Academic Unit: Institut des Biomolécules Max Mousseron - IBMM
Language: English
Resource Type: Journal article
Local Fields: hal-03564436