Novel indolizine derivatives with unprecedented ...
Type de document :
Article dans une revue scientifique
PMID :
URL permanente :
Titre :
Novel indolizine derivatives with unprecedented inhibitory activity on human farnesyltransferase
Auteur(s) :
Dumea, Carmen [Auteur]
Belei, Dalila [Auteur]
Ghinet, Alina [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Bicu, Elena [Auteur]
Belei, Dalila [Auteur]
Ghinet, Alina [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Bicu, Elena [Auteur]
Titre de la revue :
Bioorganic & Medicinal Chemistry Letters
Nom court de la revue :
Bioorg. Med. Chem. Lett.
Numéro :
24
Pagination :
5777-5781
Date de publication :
2014-12-15
ISSN :
0960-894X
Mot(s)-clé(s) en anglais :
Indolizine
Propargyl amide
Butynyl ester
Propargyl ester
Activated ester
Farnesyltransferase inhibitor
Propargyl amide
Butynyl ester
Propargyl ester
Activated ester
Farnesyltransferase inhibitor
Discipline(s) HAL :
Sciences du Vivant [q-bio]
Résumé en anglais : [en]
The rational structural modification of new substituted indolizin-3-yl(phenyl)methanones 1a-i, 2a-i and 3a-i has greatly improved human farnesyltransferase inhibition. The para-bromophenyl analog 2f bearing an ester unit ...
Lire la suite >The rational structural modification of new substituted indolizin-3-yl(phenyl)methanones 1a-i, 2a-i and 3a-i has greatly improved human farnesyltransferase inhibition. The para-bromophenyl analog 2f bearing an ester unit on the indolizine ring demonstrates the highest inhibition potential, with IC50 value of 1.3±0.2 μM. The amidic series 1a-i proves to be the most promising for future modulations, particularly at the triple bond level.Lire moins >
Lire la suite >The rational structural modification of new substituted indolizin-3-yl(phenyl)methanones 1a-i, 2a-i and 3a-i has greatly improved human farnesyltransferase inhibition. The para-bromophenyl analog 2f bearing an ester unit on the indolizine ring demonstrates the highest inhibition potential, with IC50 value of 1.3±0.2 μM. The amidic series 1a-i proves to be the most promising for future modulations, particularly at the triple bond level.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 :
2019-05-17T13:14:34Z