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]

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 >

Audience :

Internationale

Popular science :

Non

Administrative institution(s) :

CHU Lille
Inserm
Université de Lille

Collections :

• Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement (RID-AGE) - U1167
• Institut de Recherche Translationnelle sur l'Inflammation (INFINITE) - U1286

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