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EnglishKiteplatin, the neglected drug analogous of cisplatin but containing cis-1,4-DACH in place of the two ammines, has been recently reevaluated for its activity against cisplatin- and oxaliplatin-resistant tumors, in particular colo-rectal cancer. With the aim of further improving the pharmacological activity of this drug, Pt(IV) prodrugs were derived by addition of two, differently substituted, benzoate groups in axial positions (X-ray structure). The cytotoxic activity of both compounds resulted markedly potentiated reaching nanomolar concentration against a wide panel of human cancer cells. The ability of benzoate ligands to enhance the activity of kiteplatin most likely originates from their lipophilicity promoting a higher drug accumulation in cancer cells; however, it is to be noted that the increase in pharmacological effect is far greater than the increase in cellular uptake. Overcoming cisplatin- and oxaliplatin-resistance by kiteplatin derivatives appears to relate to the inability of membrane extrusion pumps to remove active Pt species from tumor cells.
| Titolo: | Cytotoxicity-boosting of kiteplatin by Pt(IV) prodrugs with axial benzoate ligands | |
| Autori: | NATILE, Giovanni (Corresponding) | |
| Data di pubblicazione: | 2016 | |
| Rivista: | ||
| Handle: | http://hdl.handle.net/11586/165520 | |
| Appare nelle tipologie: | 1.1 Articolo in rivista |
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| File | Descrizione | Tipologia | Licenza | |
|---|---|---|---|---|
| JInorgBio_2016_ 160_85_93.pdf | Articolo principale | Documento in Versione Editoriale | NON PUBBLICO - Accesso privato/ristretto | Administrator Richiedi una copia |
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