DESIGN, SYNTHESIS AND EXPERIMENTAL VALIDATION OF NOVEL HUMAN CARBONIC ANHYDRASE IX INHIBITORS
| Autoři | |
|---|---|
| Rok publikování | 2025 |
| Druh | Další prezentace na konferencích |
| Fakulta / Pracoviště MU | |
| Citace | |
| Popis | This study presents the design, synthesis and biological evaluation of a new series of 1,3,5-triazinyl benzenesulfonamide derivatives incorporating substituted piperazines, aminobenzenes, or adamantane moieties. The compounds were tested for inhibitory activity against human carbonic anhydrase isoenzymes II and IX, aiming for selectivity towards the latter, cancer associated isoenzyme IX, on the basis of an initial molecular docking screening. Several compounds showed inhibitory activity and selectivity exceeding that of the clinical benchmark acetazolamide and the drug candidate SLC-0111. The compound´s inhibition constants were determined using stop-flow spectrophotometry in an updated approach, which enables accurate K I determination with higher throughput. |
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