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

…, A Maresca, S Thibaudeau, CT Supuran

Index: Liu, Fei; Martin-Mingot, Agnes; Lecornue; Jouannetaud, Marie-Paule; Maresca, Alfonso; Thibaudeau, Sebastien; Supuran, Claudiu T. Journal of Enzyme Inhibition and Medicinal Chemistry, 2012 ,  vol. 27,  # 6  p. 886 - 891

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Citation Number: 65

Abstract

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.