Exploring isoxazoles and pyrrolidinones ...
Document type :
Article dans une revue scientifique
DOI :
PMID :
Permalink :
Title :
Exploring isoxazoles and pyrrolidinones decorated with the 4,6-dimethoxy-1,3,5-triazine unit as human farnesyltransferase inhibitors.
Author(s) :
Lucescu, Liliana [Auteur]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center (LIRIC) - U995
Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement (RID-AGE) - U1167
JUNIA [JUNIA]
Shova, Sergiu [Auteur]
Magnez, Romain [Auteur]
Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer - U837 [JPArc]
Thuru, Xavier [Auteur]
Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer - U837 [JPArc]
Centre de recherche Jean-Pierre Aubert-Neurosciences et Cancer
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Rigo, Benoit [Auteur]
JUNIA [JUNIA]
498252|||Lille Inflammation Research International Center - U 995 [LIRIC]
523045|||Facteurs de Risque et Déterminants Moléculaires des Maladies liées au Vieillissement - U 1167 [RID-AGE]
Belei, Dalila [Auteur]
Dubois, Joelle [Auteur]
Bicu, Elena [Auteur]
Ghinet, Alina [Auteur]
Lille Inflammation Research International Center (LIRIC) - U995
Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement (RID-AGE) - U1167
JUNIA [JUNIA]
Shova, Sergiu [Auteur]
Magnez, Romain [Auteur]
Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer - U837 [JPArc]
Thuru, Xavier [Auteur]
Centre de Recherche Jean-Pierre AUBERT Neurosciences et Cancer - U837 [JPArc]
Centre de recherche Jean-Pierre Aubert-Neurosciences et Cancer
Farce, Amaury [Auteur]
Lille Inflammation Research International Center - U 995 [LIRIC]
Rigo, Benoit [Auteur]
JUNIA [JUNIA]
498252|||Lille Inflammation Research International Center - U 995 [LIRIC]
523045|||Facteurs de Risque et Déterminants Moléculaires des Maladies liées au Vieillissement - U 1167 [RID-AGE]
Belei, Dalila [Auteur]
Dubois, Joelle [Auteur]
Bicu, Elena [Auteur]
Journal title :
Archiv der Pharmazie / Chemistry in Life Sciences
Abbreviated title :
Arch. Pharm. (Weinheim)
Volume number :
352
Pages :
1800227
Publication date :
2019-05
ISSN :
1521-4184
HAL domain(s) :
Sciences du Vivant [q-bio]
English abstract : [en]
Unprecedented triazinyl-isoxazoles were afforded via an effective cycloaddition reaction between nitrile oxides and the scarcely described 2-ethynyl-4,6-dimethoxy-1,3,5-triazine as dipolarophile. The biological evaluation ...
Show more >Unprecedented triazinyl-isoxazoles were afforded via an effective cycloaddition reaction between nitrile oxides and the scarcely described 2-ethynyl-4,6-dimethoxy-1,3,5-triazine as dipolarophile. The biological evaluation of the newly synthesized compounds showed that the inhibition of human farnesyltransferase by zinc complexation could be improved with triazine-isoxazole moieties. The replacement of the isoxazole unit by a pyrrolidin-2-one was detrimental to the inhibitory activity while the pyrrolidin-2-thione derivatives conserved the biological potential. The potential of selected compounds to disrupt protein farnesylation in Chinese hamster ovary (CHO) cells transfected with pEGFP-CAAX was also evaluated.Show less >
Show more >Unprecedented triazinyl-isoxazoles were afforded via an effective cycloaddition reaction between nitrile oxides and the scarcely described 2-ethynyl-4,6-dimethoxy-1,3,5-triazine as dipolarophile. The biological evaluation of the newly synthesized compounds showed that the inhibition of human farnesyltransferase by zinc complexation could be improved with triazine-isoxazole moieties. The replacement of the isoxazole unit by a pyrrolidin-2-one was detrimental to the inhibitory activity while the pyrrolidin-2-thione derivatives conserved the biological potential. The potential of selected compounds to disrupt protein farnesylation in Chinese hamster ovary (CHO) cells transfected with pEGFP-CAAX was also evaluated.Show less >
Audience :
Internationale
Popular science :
Non
Administrative institution(s) :
CHU Lille
Inserm
Université de Lille
Inserm
Université de Lille
Collections :
Research team(s) :
Therapeutic innovation targetting inflammation
Submission date :
2019-05-17T13:14:48Z
2021-06-15T12:51:06Z
2024-01-30T11:34:08Z
2024-01-30T11:35:28Z
2024-01-30T11:39:31Z
2021-06-15T12:51:06Z
2024-01-30T11:34:08Z
2024-01-30T11:35:28Z
2024-01-30T11:39:31Z