1. Chromene-Containing Aromatic Sulfonamides with Carbonic Anhydrase Inhibitory Properties
- Author
-
Sergii Slyvchuk, Mariana Pinteala, Victor Kartsev, Claudiu T. Supuran, Athina Geronikaki, Anthi Petrou, Andrea Angeli, Volodymyr Brovarets, and Stepan G. Pilyo
- Subjects
Models, Molecular ,Gene isoform ,QH301-705.5 ,carbonic anhydrase ,010402 general chemistry ,Inhibitory postsynaptic potential ,01 natural sciences ,Article ,Catalysis ,Inorganic Chemistry ,Structure-Activity Relationship ,Catalytic Domain ,Carbonic anhydrase ,inhibitors ,Humans ,Benzopyrans ,Biology (General) ,Physical and Theoretical Chemistry ,Carbonic Anhydrase Inhibitors ,QD1-999 ,Molecular Biology ,Spectroscopy ,Carbonic Anhydrases ,Sulfonamides ,metalloenzymes ,Molecular Structure ,biology ,010405 organic chemistry ,Chemistry ,Chromene ,Organic Chemistry ,Active site ,General Medicine ,Transmembrane protein ,0104 chemical sciences ,Computer Science Applications ,Cytosol ,Biochemistry ,biology.protein - Abstract
Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO2 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.
- Published
- 2021
- Full Text
- View/download PDF