Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties

Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO(2) hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological conditions. A series of chromene-based sulfonamides were synthesized and tested as possible CA inhibitors....

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Autores principales: Angeli, Andrea, Kartsev, Victor, Petrou, Anthi, Pinteala, Mariana, Brovarets, Volodymyr, Slyvchuk, Sergii, Pilyo, Stepan, Geronikaki, Athina, Supuran, Claudiu T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8150913/
https://www.ncbi.nlm.nih.gov/pubmed/34064890
http://dx.doi.org/10.3390/ijms22105082
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author Angeli, Andrea
Kartsev, Victor
Petrou, Anthi
Pinteala, Mariana
Brovarets, Volodymyr
Slyvchuk, Sergii
Pilyo, Stepan
Geronikaki, Athina
Supuran, Claudiu T.
author_facet Angeli, Andrea
Kartsev, Victor
Petrou, Anthi
Pinteala, Mariana
Brovarets, Volodymyr
Slyvchuk, Sergii
Pilyo, Stepan
Geronikaki, Athina
Supuran, Claudiu T.
author_sort Angeli, Andrea
collection PubMed
description Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO(2) hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological conditions. A series of chromene-based sulfonamides were synthesized and tested as possible CA inhibitors. Their inhibitory activity was assessed against the cytosolic human isoforms hCA I, hCA II and the transmembrane hCA IX and XII. Several of the investigated derivatives showed interesting inhibition activity towards the tumor associate isoforms hCA IX and hCA XII. Furthermore, computational procedures were used to investigate the binding mode of this class of compounds, within the active site of hCA IX.
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spelling pubmed-81509132021-05-27 Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties Angeli, Andrea Kartsev, Victor Petrou, Anthi Pinteala, Mariana Brovarets, Volodymyr Slyvchuk, Sergii Pilyo, Stepan Geronikaki, Athina Supuran, Claudiu T. Int J Mol Sci Article Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO(2) hydration in all living organisms, being actively involved in the regulation of a plethora of patho/physiological conditions. A series of chromene-based sulfonamides were synthesized and tested as possible CA inhibitors. Their inhibitory activity was assessed against the cytosolic human isoforms hCA I, hCA II and the transmembrane hCA IX and XII. Several of the investigated derivatives showed interesting inhibition activity towards the tumor associate isoforms hCA IX and hCA XII. Furthermore, computational procedures were used to investigate the binding mode of this class of compounds, within the active site of hCA IX. MDPI 2021-05-11 /pmc/articles/PMC8150913/ /pubmed/34064890 http://dx.doi.org/10.3390/ijms22105082 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Angeli, Andrea
Kartsev, Victor
Petrou, Anthi
Pinteala, Mariana
Brovarets, Volodymyr
Slyvchuk, Sergii
Pilyo, Stepan
Geronikaki, Athina
Supuran, Claudiu T.
Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties
title Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties
title_full Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties
title_fullStr Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties
title_full_unstemmed Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties
title_short Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties
title_sort chromene-containing aromatic sulfonamides with carbonic anhydrase inhibitory properties
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8150913/
https://www.ncbi.nlm.nih.gov/pubmed/34064890
http://dx.doi.org/10.3390/ijms22105082
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