Titre :

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

Auteur(s) :

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

Titre de la revue :

Bioorganic & Medicinal Chemistry Letters

Nom court de la revue :

Bioorg. Med. Chem. Lett.

Numéro :

24

Pagination :

3180-3185

Date de publication :

2014-07-15

ISSN :

0960-894X

Mot(s)-clé(s) en anglais :

Activated ester
Peptide coupling
Phenothiazine
Farnesyltransferase inhibitor

Discipline(s) HAL :

Sciences du Vivant [q-bio]

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

2019-05-17T13:08:45Z