Design of chalcogen-containing norepinephrines: efficient GPx mimics and strong cytotoxic agents against HeLa cells.

Future Med Chem

Departamento de Química Orgánica, Facultad de Química, Universidad de Sevilla, Apartado 1203, 41071, Seville, Spain.

Published: December 2016

Aim: Numerous chronic diseases exhibit multifactorial etiologies, so focusing on a single therapeutic target is usually an inadequate treatment; instead, multi-target drugs are preferred. Herein, a panel of phenolic thioureas and selenoureas were designed as new prototypes against multifactorial diseases concerning antioxidation and cytotoxicity, as a pro-oxidant environment is usually found in such diseases.

Results: Selenoureas were excellent antiradical agents and biomimetic catalysts of glutathione peroxidase for the scavenging of HO. They were also potent and selective cytotoxic agents against cancer cells, in particular HeLa (IC 2.77-6.13 μM), apoptosis being involved. Selenoureas also reduced oxidative stress in HeLa cells (IC= 3.76 μM).

Conclusion: Phenolic selenoureas are promising lead structures for the development of drugs targeting multifactorial diseases like cancer.

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Source
http://dx.doi.org/10.4155/fmc-2016-0139DOI Listing

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