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Issue 1, 2015
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6-Substituted 1,2-benzoxathiine-2,2-dioxides are isoform-selective inhibitors of human carbonic anhydrases IX, XII and VA

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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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Publication details

The article was received on 09 Oct 2014, accepted on 27 Oct 2014 and first published on 27 Oct 2014


Article type: Communication
DOI: 10.1039/C4OB02155J
Citation: 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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