Title :

Peptide chemistry applied to a new family of phenothiazine-containing inhibitors of human farnesyltransferase

Author(s) :

Dumitriu, Gina-Mirabela [Auteur]
Ghinet, Alina [Auteur]
Bicu, Elena [Auteur]
Rigo, Benoit [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Belei, Dalila [Auteur]

Journal title :

Bioorganic & Medicinal Chemistry Letters

Abbreviated title :

Bioorg. Med. Chem. Lett.

Volume number :

24

Pages :

3180-3185

Publication date :

2014-07-15

ISSN :

0960-894X

English keyword(s) :

Activated ester
Peptide coupling
Phenothiazine
Farnesyltransferase inhibitor

HAL domain(s) :

Sciences du Vivant [q-bio]

English abstract : [en]

Novel phenothiazine derivatives bearing an amino acid residue were synthesized via peptide chemistry, and evaluated for their inhibitory potential on human farnesyltransferase. The phenothiazine unit proved to be an important ...
Show more >Novel phenothiazine derivatives bearing an amino acid residue were synthesized via peptide chemistry, and evaluated for their inhibitory potential on human farnesyltransferase. The phenothiazine unit proved to be an important bulky unit in the structure of the synthesized inhibitors. Propargyl ester 20 bearing a tyrosine residue exhibited the best biological potential in vitro in the present study. Further syntheses and biological evaluation of phenothiazine derivatives are necessary in order to gain a full view of SAR in this family of farnesyltransferase inhibitors.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 :

2019-05-17T13:08:45Z