Design, synthesis and evaluation of N-substituted saccharin derivatives as selective inhibitors of tumor-associated carbonic anhydrase XII

M D'Ascenzio, S Carradori, C De Monte, D Secci…

Index: D'Ascenzio, Melissa; Carradori, Simone; De Monte, Celeste; Secci, Daniela; Ceruso, Mariangela; Supuran, Claudiu T. Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 6 p. 1821 - 1831

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Citation Number: 37

Abstract

Abstract A series of N-alkylated saccharin derivatives were synthesized and tested for the inhibition of four different isoforms of human carbonic anhydrase (CA, EC 4. 2.1. 1): the transmembrane tumor-associated CA IX and XII, and the cytosolic CA I and II. Most of the reported derivatives inhibited CA XII in the nanomolar/low micromolar range, hCA IX with KI s ranging between 11 and 390 nM, whereas they were inactive against both CA I (KI s> 50 ...