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Open AccessFeature PaperArticle

Diselenides and Benzisoselenazolones as Antiproliferative Agents and Glutathione-S-Transferase Inhibitors

1
Division of Organic Chemistry, Centre of Molecular and Macromolecular Studies, Polish Academy of Science, Sienkiewicza, 112, 90-363 Lodz, Poland
2
Department of Pharmacy, University of Salerno, Via G. Paolo II 132, 84084 Fisciano, Salerno, Italy
3
Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy
4
Institute of Chemistry Jan Długosz University in Częstochowa Częstochowa, 42-200 Armii Krajowej 13/15, Poland
5
Division of Bioorganic Chemistry, Centre of Molecular and Macromolecular Studies, Polish Academy of Science, Sienkiewicza, 112, 90-363 Lodz, Poland
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2019, 24(16), 2914; https://doi.org/10.3390/molecules24162914
Received: 8 July 2019 / Revised: 8 August 2019 / Accepted: 9 August 2019 / Published: 11 August 2019
(This article belongs to the Special Issue Chemistry & Health)
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. View Full-Text
Keywords: diselenide; benzisoselenazolone; breast cancer; glutathione S-transferase diselenide; benzisoselenazolone; breast cancer; glutathione S-transferase
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Krasowska, D.; Iraci, N.; Santi, C.; Drabowicz, J.; Cieslak, M.; Kaźmierczak-Barańska, J.; Palomba, M.; Królewska-Golińska, K.; Magiera, J.; Sancineto, L. Diselenides and Benzisoselenazolones as Antiproliferative Agents and Glutathione-S-Transferase Inhibitors. Molecules 2019, 24, 2914.

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