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Synthesis and biological evaluation of a ...
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Document type :
Article dans une revue scientifique
DOI :
10.1016/j.bmcl.2013.08.088
PMID :
24054122
Permalink :
http://hdl.handle.net/20.500.12210/11249
Title :
Synthesis and biological evaluation of a new series of N-ylides as protein farnesyltransferase inhibitors
Author(s) :
Abuhaie, Cristina-Maria [Auteur]
Ghinet, Alina [Auteur] refId
Farce, Amaury [Auteur] orcid refId
Dubois, Joelle [Auteur]
Rigo, Benoit [Auteur]
Bicu, Elena [Auteur]
Journal title :
Bioorganic & Medicinal Chemistry Letters
Abbreviated title :
Bioorg. Med. Chem. Lett.
Volume number :
23
Pages :
5887-5892
Publication date :
2013-11-01
ISSN :
0960-894X
English keyword(s) :
Anticancer agent
Farnesyltransferase inhibitor
Phenothiazine
N-Ylide
HAL domain(s) :
Sciences du Vivant [q-bio]
English abstract : [en]
A new family of 30 benzoylated N-ylides 4 and 5 was synthesized and evaluated for the inhibitory activity on human protein farnesyltransferase. Most of these novel compounds possessed in vitro inhibition potencies in the ...
Show more >
A new family of 30 benzoylated N-ylides 4 and 5 was synthesized and evaluated for the inhibitory activity on human protein farnesyltransferase. Most of these novel compounds possessed in vitro inhibition potencies in the micromolar range. The nature of the substituents on the pyridine and phenyl units proved to be important in determining inhibitory activity and generally, the replacement of the cyanoacrylonitrile function by a cyanoethylacrylate group decreased the biological potential on farnesyltransferase. These results completed our SAR study on this original class of N-ylides.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 :
2019-05-17T13:14:33Z
Université de Lille

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