Methylene versus carbonyl bridge in the ...
Type de document :
Article dans une revue scientifique
PMID :
URL permanente :
Titre :
Methylene versus carbonyl bridge in the structure of new tubulin polymerization inhibitors with tricyclic A-rings
Auteur(s) :
Moise, Iuliana-Monica [Auteur]
Bicu, Elena [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Rigo, Benoit [Auteur]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Bicu, Elena [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]

Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Rigo, Benoit [Auteur]
Ghinet, Alina [Auteur]

Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Titre de la revue :
Bioorganic & medicinal chemistry
Nom court de la revue :
Bioorg. Med. Chem.
Numéro :
24
Pagination :
6021-6030
Date de publication :
2016-11-15
ISSN :
0968-0896
Mot(s)-clé(s) en anglais :
Phenothiazine
Antitumor agent
9(10H)Acridone
Iminodibenzyl
Phenoxazine
Azaphenothiazine
Tubulin inhibitor
Antitumor agent
9(10H)Acridone
Iminodibenzyl
Phenoxazine
Azaphenothiazine
Tubulin inhibitor
Discipline(s) HAL :
Sciences du Vivant [q-bio]
Résumé en anglais : [en]
The phenothiazine group has been identified as a suitable A ring in the structure of tubulin polymerization inhibitors. In our search to identify more potent inhibitors, a study of different isosteric tricyclic groups as ...
Lire la suite >The phenothiazine group has been identified as a suitable A ring in the structure of tubulin polymerization inhibitors. In our search to identify more potent inhibitors, a study of different isosteric tricyclic groups as new potential A rings was first realized and permitted to identify 1-azaphenothiazine and iminodibenzyl as favorable modulations providing compounds with improved activity against tubulin. An investigation of the methylene group as the connector between the A and B rings revealed that the "CH" bridge was tolerated, improving the biological potency when the A unit was of phenothiazine, 1-azaphenothiazine or iminodibenzyl type. Molecules 6-8 and 12 showed increased biological activity in comparison to parent phenstatin 2 on COLO 205 colon cancer cell line. The most antineoplastic agent in the current study was phenothiazine 5 displaying a GI of 25nM against the melanoma MDA-MB-435 cell line.Lire moins >
Lire la suite >The phenothiazine group has been identified as a suitable A ring in the structure of tubulin polymerization inhibitors. In our search to identify more potent inhibitors, a study of different isosteric tricyclic groups as new potential A rings was first realized and permitted to identify 1-azaphenothiazine and iminodibenzyl as favorable modulations providing compounds with improved activity against tubulin. An investigation of the methylene group as the connector between the A and B rings revealed that the "CH" bridge was tolerated, improving the biological potency when the A unit was of phenothiazine, 1-azaphenothiazine or iminodibenzyl type. Molecules 6-8 and 12 showed increased biological activity in comparison to parent phenstatin 2 on COLO 205 colon cancer cell line. The most antineoplastic agent in the current study was phenothiazine 5 displaying a GI of 25nM against the melanoma MDA-MB-435 cell line.Lire moins >
Audience :
Internationale
Vulgarisation :
Non
Établissement(s) :
CHU Lille
Inserm
Université de Lille
Inserm
Université de Lille
Équipe(s) de recherche :
Therapeutic innovation targetting inflammation
Date de dépôt :
2019-05-17T13:14:41Z