Imidazopyridine-fused [1,3]diazepinones: modulations of positions 2 to 4 and their impacts on the anti-melanoma activity - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Journal of Enzyme Inhibition and Medicinal Chemistry Année : 2020

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

Résumé

A series of 19 novel pyrido-imidazodiazepinones, with modulations of positions 2, 3 and 4 of the diazepine ring were synthesised and screened for their in vitro cytotoxic activities against two melanoma cell lines (A375 and MDA-MB-435) and for their potential toxicity against NIH-3T3 non-cancerous cells. Selected compounds were also evaluated on the NCI-60 cell line panel. The SAR study revealed that the molecular volume and the cLogP of compounds modified at position 2 were significantly correlated with the activity of these compounds on melanoma cell lines. Moreover, introduction of a heterocyclic group at position 2 or an azido-alkyl chain at position 4 led to compounds displaying a significantly different activity profile on the NCI-60 cell line panel, compared to phenyl-substituted compounds at position 2 of the diazepinone. This study provides us crucial information for the development of new derivatives active against melanoma.
Fichier principal
Vignette du fichier
14756366.2020.pdf (3.3 Mo) Télécharger le fichier
Origine Fichiers éditeurs autorisés sur une archive ouverte

Dates et versions

hal-03582596 , version 1 (21-02-2022)

Licence

Identifiants

Citer

Paul Le Baccon-Sollier, Yohan Malki, Morgane Maye, Lamiaa M A Ali, Laure Lichon, et al.. Imidazopyridine-fused [1,3]diazepinones: modulations of positions 2 to 4 and their impacts on the anti-melanoma activity. Journal of Enzyme Inhibition and Medicinal Chemistry, 2020, 35, pp.935 - 949. ⟨10.1080/14756366.2020.1748024⟩. ⟨hal-03582596⟩
14 Consultations
32 Téléchargements

Altmetric

Partager

Gmail Mastodon Facebook X LinkedIn More