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New structural features of isatin dihydrothiazole hybrids for selective carbonic anhydrase inhibitorsSecci, Daniela ...Chemotherapeutic agents have remained the first-line treatment option for advanced-stage cancers when surgery or radiation therapy is not viable. Human carbonic anhydrase (hCA) isoforms IX and XII ... have been validated as anticancer targets. In particular, hCA IX is overexpressed in several solid tumor cells. As a result, selective isoform inhibitors with high potency and low toxicity are sought after. Pursuing our investigation on new scaffolds as hCA-selective inhibitors, a new series of isatin thiazolidinone hybrids has been designed and synthesized. Their biological activity and selectivity toward hCA I, hCA II, hCA IX, and hCA XII were investigated. The results revealed an inhibitory activity in the nanomolar range on carbonic anhydrases IX and XII, and the nature of substitution in positions 3 and 5 of thiazolidinone appears to be crucial for the compounds’ selectivity. Docking experiments have been applied to predict the binding mode of these new, promising derivatives.Type of material - article, component part ; adult, seriousPublish date - 2024Language - englishCOBISS.SI-ID - 204916483
Author
Secci, Daniela |
Distinto, Simona |
Onali, Alessia |
Sanna, Erica |
Lupia, Antonio |
Demuru, Laura |
Atzeni, Giulia |
Cottiglia, Filippo |
Meleddu, Rita |
Angeli, Andrea, pharmacist
Topics
Farmacevtska kemija |
enzyme inhibitors |
human carbonic anhydrase |
docking experiments |
structural elucidation |
zaviralci encimov |
humana karboanhidraza |
poskusi priklopa |
strukturna razjasnitev
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Secci, Daniela | 58611 |
Distinto, Simona | ![]() |
Onali, Alessia | ![]() |
Sanna, Erica | ![]() |
Lupia, Antonio | ![]() |
Demuru, Laura | ![]() |
Atzeni, Giulia | ![]() |
Cottiglia, Filippo | ![]() |
Meleddu, Rita | ![]() |
Angeli, Andrea, pharmacist | ![]() |
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