Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties
Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO<sub>2</sub> 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 pos...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2021-05-01
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| Series: | International Journal of Molecular Sciences |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1422-0067/22/10/5082 |
| Summary: | Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO<sub>2</sub> 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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| ISSN: | 1661-6596 1422-0067 |