Issue 1, 2015
From the journal:

Organic & Biomolecular Chemistry

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

Muhammet Tanc,ab   Fabrizio Carta,*b   Andrea Scozzafavab  and  Claudiu T. Supuran*ab  

* Corresponding authors

a Università degli Studi di Firenze, NEUROFARBA Department, Section of Pharmaceutical Chemistry, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy
E-mail: claudiu.supuran@unifi.it

b Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino (Florence), Italy
E-mail: fabrizio.carta@unifi.it

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

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Article information

DOI
https://doi.org/10.1039/C4OB02155J
Article type
Communication
Submitted
09 Oct 2014
Accepted
27 Oct 2014
First published
27 Oct 2014

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

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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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