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

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.

Keywords::

• Hypoxic tumors
• superelectrophiles
• fluorine chemistry
• sultams

Acknowledgement

We thank the region Poitou-Charentes (grant to F.Liu.), the CNRS and the University of Poitiers for financial support and an EU FP7 grant (Metoxia, to CTS).

Declaration of interest

Financial support and EU FP7 grant (Metoxia, to CTS) were provided by the region Poitou-Charentes (grant to F.Liu.), the CNRS and the University of Poitierregion. The authors report no declarations of interest.