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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)
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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. View Full-Text
Keywords: diselenide; benzisoselenazolone; breast cancer; glutathione S-transferase diselenide; benzisoselenazolone; breast cancer; glutathione S-transferase
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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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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