UNICA IRIS Institutional Research Information System
IRIS è il sistema di gestione integrata dei dati della ricerca (persone, progetti, pubblicazioni, attività) adottato dall'Università degli Studi di Cagliari dal mese di luglio 2015.
EnglishBy using SLC-0111 (4-fluorophenylureido-benzenesulfonamide), a sulfonamide carbonic anhydrase (CA, EC 4.2.1.1) inhibitor in Phase I clinical trials as an antitumor agent as lead molecule, a series of benzenesulfonamide derivatives incorporating ureido moieties was synthesized. The new compounds contain a 4-N-substituted piperazine fragment in which the ureido linker has been included, and were tested as inhibitors of the cytosolic human (h) hCA I and II isoforms, as well as the transmembrane, tumor-associated enzymes hCA IX and XII. Depending on the substitution pattern at the piperazine ring, low nanomolar inhibitors were detected against all four isoforms, making the new class of sulfonamides of interest for various pharmacologic applications.
Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity / Congiu, Cenzo; Onnis, Valentina; Deplano, Alessandro; Balboni, Gianfranco; Dedeoglu, Nurcan; Supuran, Claudiu T.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 25:18(2015), pp. 3850-3853.
| Titolo: | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity |
| Autori: | |
| Data di pubblicazione: | 2015 |
| Rivista: | |
| Citazione: | Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity / Congiu, Cenzo; Onnis, Valentina; Deplano, Alessandro; Balboni, Gianfranco; Dedeoglu, Nurcan; Supuran, Claudiu T.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 25:18(2015), pp. 3850-3853. |
| Handle: | http://hdl.handle.net/11584/113166 |
| Tipologia: | 1.1 Articolo in rivista |
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|---|---|---|---|---|
| BMCL_2015_CAI_supporting info.docx | supplementary informations | altro documento allegato | Administrator Richiedi una copia | |
| BMCL_2015_CAI_supporting info2.xlsx | supporting information 2 | altro documento allegato | Administrator Richiedi una copia | |
| BMCL 2015_CAI.pdf | Articolo principale Versione dell'editore | versione editoriale | Administrator Richiedi una copia |
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