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Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides.

作者信息

Smaine Fatma-Zohra, Winum Jean-Yves, Montero Jean-Louis, Regainia Zine, Vullo Daniela, Scozzafava Andrea, Supuran Claudiu T

机构信息

Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS-UM1-UM2 Bâtiment de Recherche Max Mousseron, Ecole Nationale Supérieure de Chimie de Montpellier, 8 rue de l'Ecole Normale, 34296 Montpellier Cedex, France.

出版信息

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5096-100. doi: 10.1016/j.bmcl.2007.07.019. Epub 2007 Jul 13.

DOI:10.1016/j.bmcl.2007.07.019
PMID:17646100
Abstract

A series of glycosyl-thioureido sulfonamides incorporating glucosamine, galactosamine, and mannosamine tails, and sulfanilamide, halogenosulfanilamide, and metanilamide heads was synthesized. Many of the new compounds showed micromolar-submicromolar affinity for the inhibition of the cytosolic isoforms I and II of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), but low nanomolar binding to the tumor-associated isozymes, CA IX and XII. The selectivity ratios for the inhibition of the tumor-associated over the cytosolic isozymes were in the range of 107-955 for the most selective such inhibitors.

摘要

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