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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Carbonic anhydrase inhibitors: Selective inhibition of the extracellular, tumor-associated isoforms IX and XII over isozymes I and II with glycosyl-thioureido-sulfonamides
Bioorganic and Medicinal Chemistry Letters, Volume 17, No. 18, Year 2007
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Description
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. © 2007 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Smaine, Fatma Zhora
France, Montpellier
Enscm Ecole Nationale Supérieure de Chimie de Montpellier
Algeria, Annaba
Université Badji Mokhtar - Annaba
Winum., Jean Yves
France, Montpellier
Enscm Ecole Nationale Supérieure de Chimie de Montpellier
Montéro, Jean Louis Georges
France, Montpellier
Enscm Ecole Nationale Supérieure de Chimie de Montpellier
Régaïnia, Zine
Algeria, Annaba
Université Badji Mokhtar - Annaba
Vullo, Daniela
Italy, Florence
Università Degli Studi Di Firenze
Scozzafava, A.
Italy, Florence
Università Degli Studi Di Firenze
Supuran, Claudiu T.
Italy, Florence
Università Degli Studi Di Firenze
Statistics
Citations: 20
Authors: 7
Affiliations: 3
Identifiers
Doi:
10.1016/j.bmcl.2007.07.019
ISSN:
0960894X
Research Areas
Cancer