Title :

Synthesis and biological evaluation of a new series of phenothiazine-containing protein farnesyltransferase inhibitors

Author(s) :

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

Journal title :

European journal of medicinal chemistry

Abbreviated title :

Eur. J. Med. Chem.

Volume number :

59

Pages :

101-110

Publication date :

2013-01-01

ISSN :

0223-5234

English keyword(s) :

Fanesyltransferase inhibitors
Ylide
Anticancer agent
Pyridin-(1H)-ylidene
Phenothiazine

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

Two new families of human farnesyltransferase inhibitors 13a-m and 14a-d, based on a phenothiazine scaffold, were synthesized. Compounds 14a and 14b were the most promising inhibitors of human farnesyltransferase with ...
Show more >Two new families of human farnesyltransferase inhibitors 13a-m and 14a-d, based on a phenothiazine scaffold, were synthesized. Compounds 14a and 14b were the most promising inhibitors of human farnesyltransferase with IC(50) values of 0.7 and 0.6 μM, respectively.Show less >

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

CHU Lille
Inserm
Université de Lille

Collections :

• Lille Inflammation Research International Center (LIRIC) - U995

Research team(s) :

Therapeutic innovation targetting inflammation

Submission date :

2019-05-17T13:14:32Z