New farnesyltransferase inhibitors in the ...
Document type :
Article dans une revue scientifique
PMID :
Permalink :
Title :
New farnesyltransferase inhibitors in the phenothiazine series
Author(s) :
Belei, Dalila [Auteur]
Dumea, Carmen [Auteur]
Samson, Alexandrina [Auteur]
Farce, Amaury [Auteur]
Dubois, Joelle [Auteur]
Bicu, Elena [Auteur]
Ghinet, Alina [Auteur]
Dumea, Carmen [Auteur]
Samson, Alexandrina [Auteur]
Farce, Amaury [Auteur]
Dubois, Joelle [Auteur]
Bicu, Elena [Auteur]
Ghinet, Alina [Auteur]
Journal title :
Bioorganic & Medicinal Chemistry Letters
Abbreviated title :
Bioorg. Med. Chem. Lett.
Volume number :
22
Pages :
4517-4522
Publication date :
2012-07-15
ISSN :
0960-894X
English keyword(s) :
Phenothiazine
Farnesyltransferase inhibitor
Triazole
Anticancer agent
Farnesyltransferase inhibitor
Triazole
Anticancer agent
HAL domain(s) :
Sciences du Vivant [q-bio]
English abstract : [en]
The biological screening of the chemical library of our Organic Chemistry Department, carried out on an automated fluorescence-based FTase assay, allowed us to discover that a phenothiazine derivative (1d) was an inhibitor ...
Show more >The biological screening of the chemical library of our Organic Chemistry Department, carried out on an automated fluorescence-based FTase assay, allowed us to discover that a phenothiazine derivative (1d) was an inhibitor of farnesyltransferase. Three new series of human farnesyltransferase inhibitors, based on a phenothiazine scaffold, were synthesized with protein farnesyltransferase inhibition potencies in the low micromolar range. Ester derivative 9d was the most active compound in these series. Four synthesized compounds were evaluated for their antiproliferative activity on a NCI-60 cancer cell line panel. The modest results obtained in this preliminary investigation showed that mixing the phenothiazine and the 1,2,3-triazole motif in the structure of a single compound can lead to new scaffolds in the field of farnesyltransferase inhibitors.Show less >
Show more >The biological screening of the chemical library of our Organic Chemistry Department, carried out on an automated fluorescence-based FTase assay, allowed us to discover that a phenothiazine derivative (1d) was an inhibitor of farnesyltransferase. Three new series of human farnesyltransferase inhibitors, based on a phenothiazine scaffold, were synthesized with protein farnesyltransferase inhibition potencies in the low micromolar range. Ester derivative 9d was the most active compound in these series. Four synthesized compounds were evaluated for their antiproliferative activity on a NCI-60 cancer cell line panel. The modest results obtained in this preliminary investigation showed that mixing the phenothiazine and the 1,2,3-triazole motif in the structure of a single compound can lead to new scaffolds in the field of farnesyltransferase inhibitors.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 :
2019-05-17T13:08:47Z