Issue 1, 2015

6-Substituted 1,2-benzoxathiine-2,2-dioxides are isoform-selective inhibitors of human carbonic anhydrases IX, XII and VA

Abstract

A series of 6-substituted 2-benzoxathiine-2,2-dioxides were synthesized starting from 2,5-dihydroxybenzaldehyde, and then screened in vitro for their inhibition properties against five human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms. All the compounds showed excellent selectivity against the mitochondrial (hCA VA) and the tumor associated (hCA IX and XII) enzymes.

Graphical abstract: 6-Substituted 1,2-benzoxathiine-2,2-dioxides are isoform-selective inhibitors of human carbonic anhydrases IX, XII and VA

Supplementary files

Article information

Article type
Communication
Submitted
09 Oct 2014
Accepted
27 Oct 2014
First published
27 Oct 2014

Org. Biomol. Chem., 2015,13, 77-80

6-Substituted 1,2-benzoxathiine-2,2-dioxides are isoform-selective inhibitors of human carbonic anhydrases IX, XII and VA

M. Tanc, F. Carta, A. Scozzafava and C. T. Supuran, Org. Biomol. Chem., 2015, 13, 77 DOI: 10.1039/C4OB02155J

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