Titre :

Synthesis and biological evaluation of a new series of N-ylides as protein farnesyltransferase inhibitors

Auteur(s) :

Abuhaie, Cristina-Maria [Auteur]
Ghinet, Alina [Auteur]
Farce, Amaury [Auteur]
Dubois, Joelle [Auteur]
Rigo, Benoit [Auteur]
Bicu, Elena [Auteur]

Titre de la revue :

Bioorganic & Medicinal Chemistry Letters

Nom court de la revue :

Bioorg. Med. Chem. Lett.

Numéro :

23

Pagination :

5887-5892

Date de publication :

2013-11-01

ISSN :

0960-894X

Mot(s)-clé(s) en anglais :

Anticancer agent
Farnesyltransferase inhibitor
Phenothiazine
N-Ylide

Discipline(s) HAL :

Sciences du Vivant [q-bio]

Résumé en anglais : [en]

A new family of 30 benzoylated N-ylides 4 and 5 was synthesized and evaluated for the inhibitory activity on human protein farnesyltransferase. Most of these novel compounds possessed in vitro inhibition potencies in the ...
Lire la suite >A new family of 30 benzoylated N-ylides 4 and 5 was synthesized and evaluated for the inhibitory activity on human protein farnesyltransferase. Most of these novel compounds possessed in vitro inhibition potencies in the micromolar range. The nature of the substituents on the pyridine and phenyl units proved to be important in determining inhibitory activity and generally, the replacement of the cyanoacrylonitrile function by a cyanoethylacrylate group decreased the biological potential on farnesyltransferase. These results completed our SAR study on this original class of N-ylides.Lire moins >

Audience :

Internationale

Vulgarisation :

Non

Établissement(s) :

CHU Lille
Inserm
Université de Lille

Collections :

• Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286

Équipe(s) de recherche :

Therapeutic innovation targetting inflammation

Date de dépôt :

2019-05-17T13:14:33Z