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New indolizine-chalcones as potent inhibitors ...
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Document type :
Article dans une revue scientifique
DOI :
10.1016/j.bmcl.2016.05.074
PMID :
27282741
Permalink :
http://hdl.handle.net/20.500.12210/11278
Title :
New indolizine-chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation
Author(s) :
Moise, Iuliana-Monica [Auteur]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center (LIRIC) - U995
Lille Inflammation Research International Center (LIRIC) - U995
Belei, Dalila [Auteur]
Dubois, Joelle [Auteur]
Farce, Amaury [Auteur]
Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286
Bicu, Elena [Auteur]
Journal title :
Bioorganic & Medicinal Chemistry Letters
Abbreviated title :
Bioorg. Med. Chem. Lett.
Volume number :
26
Pages :
3730-3734
Publication date :
2016-08-01
ISSN :
0960-894X
English keyword(s) :
Antitumor agent
Phenothiazine
Farnesyltransferase inhibitor
Chalcone
Indolizine
HAL domain(s) :
Sciences du Vivant [q-bio]
English abstract : [en]
A new family of indolizine-chalcones was designed, synthesized and screened for the inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents. The most active compound was phenothiazine ...
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A new family of indolizine-chalcones was designed, synthesized and screened for the inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents. The most active compound was phenothiazine 2a, exhibiting an IC50 value in the low nanomolar range, similar to that of known FTI-276, highly potent farnesyltransferase inhibitor. The newly synthesized indolizine-chalcones 2a-d constitute the most efficient inhibitors of farnesyltransferase bearing a phenothiazine unit known to date.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 :
2019-05-17T13:14:40Z
Université de Lille

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