Title :

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

Author(s) :

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

Journal title :

Bioorganic & Medicinal Chemistry Letters

Abbreviated title :

Bioorg. Med. Chem. Lett.

Volume number :

23

Pages :

5887-5892

Publication date :

2013-11-01

ISSN :

0960-894X

English keyword(s) :

Anticancer agent
Farnesyltransferase inhibitor
Phenothiazine
N-Ylide

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [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 ...
Show more >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.Show less >

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

CHU Lille
Inserm
Université de Lille

Collections :

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

Research team(s) :

Therapeutic innovation targetting inflammation

Submission date :

2019-05-17T13:14:33Z