1. Diselenides and Benzisoselenazolones as Antiproliferative Agents and Glutathione-S-Transferase Inhibitors.
- Author
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Krasowska, Dorota, Iraci, Nunzio, Santi, Claudio, Drabowicz, Józef, Cieslak, Marcin, Kaźmierczak-Barańska, Julia, Palomba, Martina, Królewska-Golińska, Karolina, Magiera, Jakub, and Sancineto, Luca
- Subjects
GLUTATHIONE transferase ,CANCER cells ,CELL lines ,LEAD compounds ,ENZYMES - 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. [ABSTRACT FROM AUTHOR]
- Published
- 2019
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