A series of benzofused sultams and fluorinated benzenesulfonamides were synthesized in superacid HF/SbF(5) 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.
Carbonic Anhydrases inhibitory effects of new benzenesulfonamides synthesized by using superacid chemistry / F. Liu;A. Martin-Mingot;F. Lecornué;M. Jouannetaud;A. Maresca;S. Thibaudeau;C. T. Supuran. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - STAMPA. - (2011), pp. 0-0. [10.3109/14756366.2011.638921]
Carbonic Anhydrases inhibitory effects of new benzenesulfonamides synthesized by using superacid chemistry.
SUPURAN, CLAUDIU TRANDAFIR
2011
Abstract
A series of benzofused sultams and fluorinated benzenesulfonamides were synthesized in superacid HF/SbF(5) 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.
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