Novel indolizine derivatives with unprecedented ...
Document type :
Article dans une revue scientifique
PMID :
Permalink :
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]
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
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 >
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
Inserm
Université de Lille
Research team(s) :
Therapeutic innovation targetting inflammation
Submission date :
2019-05-17T13:14:34Z