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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Detalles Bibliográficos
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
Descripción
Sumario: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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