Titre :

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

Auteur(s) :

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

Titre de la revue :

Bioorganic & Medicinal Chemistry Letters

Nom court de la revue :

Bioorg. Med. Chem. Lett.

Numéro :

22

Pagination :

6896-6902

Date de publication :

2012-11-15

ISSN :

0960-894X

Mot(s)-clé(s) en anglais :

Pyrazole
Pyrazoline
Phenothiazine
Farnesyltransferase inhibitor
Cytostatic agent
Acylhydrazone

Discipline(s) HAL :

Sciences du Vivant [q-bio]

Résumé en anglais : [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, ...
Lire la suite >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.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 :

2019-05-17T13:14:31Z