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Peptide chemistry applied to a new family ...
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Document type :
Article dans une revue scientifique
DOI :
10.1016/j.bmcl.2014.04.102
PMID :
24856060
Permalink :
http://hdl.handle.net/20.500.12210/11229
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 :
  • Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
Research team(s) :
Therapeutic innovation targetting inflammation
Submission date :
2019-05-17T13:08:45Z
Université de Lille

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