Cyclopropyl-tryptamine analogues: synthesis and biological evaluation as 5-HT(6) receptor ligands.
Fiche publication
Date publication
janvier 2013
Auteurs
Membres identifiés du Cancéropôle Est :
Pr SAPI Janos, Dr GERARD Stéphane
Tous les auteurs :
Szalata C, Szymoniak J, Fabis F, Butt-Gueulle S, Rault S, Bertus P, Gerard S, Sapi J
Lien Pubmed
Résumé
Conformational restrictions: Based on the pharmacophore model for 5-HT(6) receptor ligands (shown), tryptamine analogues bearing a cyclopropyl ring on the alpha-position of the tryptamine side chain were synthesized and evaluated against 5-HT receptors. N,N-Dimethyl-1-arylsulfonyltryptamine derivatives exhibited promising selectivity for 5-HT(6) over 5-HT(1a) and 5-HT(4) receptors and interesting activity against 5-HT(6) (K(i) = approximately 0.15 muM; IC(50) = approximately 0.20 muM).
Référence
ChemMedChem. 2013 Jan;8(1):70-3