Title :

Novel indolizine derivatives with unprecedented inhibitory activity on human farnesyltransferase

Author(s) :

Dumea, Carmen [Auteur]
Belei, Dalila [Auteur]
Ghinet, Alina [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Bicu, Elena [Auteur]

Journal title :

Bioorganic & Medicinal Chemistry Letters

Abbreviated title :

Bioorg. Med. Chem. Lett.

Volume number :

24

Pages :

5777-5781

Publication date :

2014-12-15

ISSN :

0960-894X

English keyword(s) :

Indolizine
Propargyl amide
Butynyl ester
Propargyl ester
Activated ester
Farnesyltransferase inhibitor

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

The rational structural modification of new substituted indolizin-3-yl(phenyl)methanones 1a-i, 2a-i and 3a-i has greatly improved human farnesyltransferase inhibition. The para-bromophenyl analog 2f bearing an ester unit ...
Show more >The rational structural modification of new substituted indolizin-3-yl(phenyl)methanones 1a-i, 2a-i and 3a-i has greatly improved human farnesyltransferase inhibition. The para-bromophenyl analog 2f bearing an ester unit on the indolizine ring demonstrates the highest inhibition potential, with IC50 value of 1.3±0.2 μM. The amidic series 1a-i proves to be the most promising for future modulations, particularly at the triple bond level.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 :

2019-05-17T13:14:34Z