Exploring isoxazoles and pyrrolidinones decorated with the 4,6‐dimethoxy‐1,3,5‐triazine unit as human farnesyltransferase inhibitors | Zendy

Lucescu Liliana | Zendy; Ghinet Alina | Zendy; Shova Sergiu | Zendy; Magnez Romain | Zendy; Thuru Xavier | Zendy; Farce Amaury | Zendy; Rigo Benoît | Zendy; Belei Dalila | Zendy; Dubois Joëlle | Zendy; Bîcu Elena | Zendy

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Exploring isoxazoles and pyrrolidinones decorated with the 4,6‐dimethoxy‐1,3,5‐triazine unit as human farnesyltransferase inhibitors

Author(s) -

Lucescu Liliana,

Ghinet Alina,

Shova Sergiu,

Magnez Romain,

Thuru Xavier,

Farce Amaury,

Rigo Benoît,

Belei Dalila,

Dubois Joëlle,

Bîcu Elena

Publication year - 2019

Publication title -

archiv der pharmazie

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.468

H-Index - 61

eISSN - 1521-4184

pISSN - 0365-6233

DOI - 10.1002/ardp.201800227

Subject(s) - farnesyltransferase , isoxazole , pyrrolidinones , chinese hamster ovary cell , chemistry , cycloaddition , triazine , nitrile , combinatorial chemistry , 1,3,5 triazine , stereochemistry , organic chemistry , biochemistry , catalysis , prenylation , enzyme , receptor

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.

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