Literature DB >> 27871038

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

Virginie Bellet1, Laure Lichon1, Dominique P Arama1, Audrey Gallud1, Vincent Lisowski1, Ludovic T Maillard1, Marcel Garcia1, Jean Martinez1, Nicolas Masurier2.   

Abstract

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. Copyright Â
© 2016 Elsevier Masson SAS. All rights reserved.

Entities:  

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

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Year:  2016        PMID: 27871038     DOI: 10.1016/j.ejmech.2016.11.023

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  2 in total

1.  Imidazopyridine-fused [1,3]diazepinones: modulations of positions 2 to 4 and their impacts on the anti-melanoma activity.

Authors:  Paul Le Baccon-Sollier; Yohan Malki; Morgane Maye; Lamiaa M A Ali; Laure Lichon; Pierre Cuq; Laure-Anaïs Vincent; Nicolas Masurier
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

2.  Design, synthesis and molecular mechanisms of novel dual inhibitors of heat shock protein 90/phosphoinositide 3-kinase alpha (Hsp90/PI3Kα) against cutaneous melanoma.

Authors:  Feifei Qin; Yali Wang; Xian Jiang; Yujia Wang; Nan Zhang; Xiang Wen; Lian Wang; Qinglin Jiang; Gu He
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

  2 in total

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