NOVEL INHIBITORS OF HUMAN CARBONIC ANHYDRASE
| Autoři | |
|---|---|
| Rok publikování | 2024 |
| Druh | Další prezentace na konferencích |
| Fakulta / Pracoviště MU | |
| Citace | |
| Popis | Carbonic anhydrases (CA, EC 4.2.1.1) are metalloenzymes catalyzing the reversible hydration of CO2, thereby affecting the pH and related physiological processes in various organisms. In human bodies, 15 different isoforms of CAs can be found, including two tumor-associated: hCA IX and hCA XII (human CA). These two isoforms are responsible for up-regulated metabolism, growth, and survival of cancer cells. They are involved in spreading metastasis, and correlated with resistance towards chemotherapy or radiotherapy.1 Given the above, it is clear that CA inhibitors are very promising compounds in cancer treatment. However, for now, their crucial limitation is their selectivity towards specific isoenzymes. A new series of inhibitors of tumor-associated CA was designed and synthesized, specifically 1,3,5-triazines containing aminobenzenesulfonamide, piperazine, aniline, and other structural moieties. New compounds' inhibitory activity and selectivity were determined against hCA IX, hCA XII, and hCA II. |
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