Title :

Synthesis and biological evaluation of new phenothiazine derivatives bearing a pyrazole unit as protein farnesyltransferase inhibitors

Author(s) :

Baciu-Atudosie, Lavinia [Auteur]
Ghinet, Alina [Auteur]
Farce, Amaury [Auteur]
Dubois, Joelle [Auteur]
Belei, Dalila [Auteur]
Bicu, Elena [Auteur]

Journal title :

Bioorganic & Medicinal Chemistry Letters

Abbreviated title :

Bioorg. Med. Chem. Lett.

Volume number :

22

Pages :

6896-6902

Publication date :

2012-11-15

ISSN :

0960-894X

English keyword(s) :

Pyrazole
Pyrazoline
Phenothiazine
Farnesyltransferase inhibitor
Cytostatic agent
Acylhydrazone

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

A new family of protein farnesyltransferase inhibitors, based on a phenothiazine scaffold, was designed and synthesized. The biological evaluation of these products showed that compounds 28 and 30 were the most active, ...
Show more >A new family of protein farnesyltransferase inhibitors, based on a phenothiazine scaffold, was designed and synthesized. The biological evaluation of these products showed that compounds 28 and 30 were the most active, with protein farnesyltransferase inhibition potencies in the low micromolar range. Compounds were also evaluated for their antiproliferative activity on a NCI-60 cancer cell line panel. Indenopyrazole 30 exhibited the most potent in vitro cytostatic activity inhibiting the growth of HCT-116, LOX IMVI and SK-MEL-5 cell lines.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 :

2019-05-17T13:14:31Z