New indolizine-chalcones as potent inhibitors ...
Type de document :
Article dans une revue scientifique
PMID :
URL permanente :
Titre :
New indolizine-chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation
Auteur(s) :
Moise, Iuliana-Monica [Auteur]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Belei, Dalila [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Bicu, Elena [Auteur]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Belei, Dalila [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Lille Inflammation Research International Center - U 995 [LIRIC]
Bicu, Elena [Auteur]
Titre de la revue :
Bioorganic & Medicinal Chemistry Letters
Nom court de la revue :
Bioorg. Med. Chem. Lett.
Numéro :
26
Pagination :
3730-3734
Date de publication :
2016-08-01
ISSN :
0960-894X
Mot(s)-clé(s) en anglais :
Antitumor agent
Phenothiazine
Farnesyltransferase inhibitor
Chalcone
Indolizine
Phenothiazine
Farnesyltransferase inhibitor
Chalcone
Indolizine
Discipline(s) HAL :
Sciences du Vivant [q-bio]
Résumé en anglais : [en]
A new family of indolizine-chalcones was designed, synthesized and screened for the inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents. The most active compound was phenothiazine ...
Lire la suite >A new family of indolizine-chalcones was designed, synthesized and screened for the inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents. The most active compound was phenothiazine 2a, exhibiting an IC50 value in the low nanomolar range, similar to that of known FTI-276, highly potent farnesyltransferase inhibitor. The newly synthesized indolizine-chalcones 2a-d constitute the most efficient inhibitors of farnesyltransferase bearing a phenothiazine unit known to date.Lire moins >
Lire la suite >A new family of indolizine-chalcones was designed, synthesized and screened for the inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents. The most active compound was phenothiazine 2a, exhibiting an IC50 value in the low nanomolar range, similar to that of known FTI-276, highly potent farnesyltransferase inhibitor. The newly synthesized indolizine-chalcones 2a-d constitute the most efficient inhibitors of farnesyltransferase bearing a phenothiazine unit known to date.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 :
2019-05-17T13:14:40Z