Title :

New indolizine-chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation

Author(s) :

Moise, Iuliana-Monica [Auteur]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center (LIRIC) - U995
Lille Inflammation Research International Center (LIRIC) - U995
Belei, Dalila [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Lille Inflammation Research International Center (LIRIC) - U995
Lille Inflammation Research International Center (LIRIC) - U995
Bicu, Elena [Auteur]

Journal title :

Bioorganic & Medicinal Chemistry Letters

Abbreviated title :

Bioorg. Med. Chem. Lett.

Volume number :

26

Pages :

3730-3734

Publication date :

2016-08-01

ISSN :

0960-894X

English keyword(s) :

Antitumor agent
Phenothiazine
Farnesyltransferase inhibitor
Chalcone
Indolizine

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

A new family of indolizine-chalcones was designed, synthesized and screened for the inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents. The most active compound was phenothiazine ...
Show more >A new family of indolizine-chalcones was designed, synthesized and screened for the inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents. The most active compound was phenothiazine 2a, exhibiting an IC50 value in the low nanomolar range, similar to that of known FTI-276, highly potent farnesyltransferase inhibitor. The newly synthesized indolizine-chalcones 2a-d constitute the most efficient inhibitors of farnesyltransferase bearing a phenothiazine unit known to date.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 :

2019-05-17T13:14:40Z