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EnglishA series of variously functionalized selenium-containing compounds were purposely synthesized and evaluated against a panel of cancer cell lines. Most of the compounds showed an interesting cytotoxicity profile with compound 5 showing a potent activity on MCF7 cells. The ethyl amino derivative 5 acts synergistically with cis-platin and inhibits the GST enzyme with a potency that well correlates with the cytotoxicity observed in MCF7 cells. A computational analysis suggests a possible binding mode on the GST enzyme. As the main outcome of the present study, the ethyl amino derivative 5 emerged as a valid lead compound for further, future developments.
| Titolo: | Diselenides and benzisoselenazolones as antiproliferative agents and glutathione-S-transferase inhibitors |
| Autori: | IRACI, Nunzio (Co-primo) |
| Data di pubblicazione: | 2019 |
| Rivista: | |
| Abstract: | A series of variously functionalized selenium-containing compounds were purposely synthesized and evaluated against a panel of cancer cell lines. Most of the compounds showed an interesting cytotoxicity profile with compound 5 showing a potent activity on MCF7 cells. The ethyl amino derivative 5 acts synergistically with cis-platin and inhibits the GST enzyme with a potency that well correlates with the cytotoxicity observed in MCF7 cells. A computational analysis suggests a possible binding mode on the GST enzyme. As the main outcome of the present study, the ethyl amino derivative 5 emerged as a valid lead compound for further, future developments. |
| Handle: | http://hdl.handle.net/11570/3189065 |
| Appare nelle tipologie: | 14.a.1 Articolo su rivista |
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|---|---|---|---|---|
| molecules-24-02914(1).pdf | Versione Editoriale (PDF) |  | Open Access Visualizza/Apri |
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