Carbonic Anhydrases inhibitory effects of new benzenesulfonamides synthesized by using superacid chemistry

F. Lin , A. Martin-Mingot , F. Lecornué , M.P. Jouannetaud , A. Maresca (1) , S. Thibaudeau (2) , Ct Supuran (1)

1 UniFI - Università degli Studi di Firenze = University of Florence = Université de Florence
2 OrgaSynth - Synthèse organique [E5 – IC2MP équipe 5]

A series of benzofused sultams and fluorinated benzenesulfonamides were synthesized in superacid HF/SbF5 from simple N-allylic derivatives. Almost all of these original compounds showed micromolar inhibitory activities against carbonic anhydrases I and II. The fluorinated derivatives inhibit better the tumor-associated isoforms IX and XII, and one of the tested compounds showed inhibition in the nanomolar range.

Domaines: Catalyse; Chimie organique; Autre

F. Lin, A. Martin-Mingot, F. Lecornué, M.P. Jouannetaud, A. Maresca, et al.. Carbonic Anhydrases inhibitory effects of new benzenesulfonamides synthesized by using superacid chemistry. Journal of Enzyme Inhibition and Medicinal Chemistry, 2012, 27 (6), pp.886-891. ⟨10.3109/14756366.2011.638921⟩. ⟨hal-00823328⟩