US EPA

4332707 

Journal Article 

Chalcogen-containing phenolics as antiproliferative agents 

Begines, P; Oliete, A; López, Ó; Maya, I; Plata, GB; Padrón, JM; Fernández-Bolaños, JG 

2018 

Yes 

Future Medicinal Chemistry
ISSN: 1756-8919 

FUTURE SCI LTD 

LONDON 

10 

3 

319-334 

English 

29400087 

10.4155/fmc-2017-0053 

WOS:000425887600005 

AIM: The increasing number of cancer cases has stimulated researchers to seek for novel approaches. We have combined two bioactive moieties: a polyphenolic scaffold and an organoselenium motif. Four different families (isothiocyanates/thioureas, and their selenium isosters) derived from dopamine, (±)-norepinephrine and R-epinephrine were accessed.

RESULTS: Heterocumulenes derived from dopamine and β-O-methylnoradrenaline were strong antiproliferative agents (GI50<10 μM). Selenoureas derived from β-O-methylnoradrenaline bearing electron-withdrawing groups (halogen, -NO2, -Ph) on the phenyl ring, were also strong antiproliferative agents, besides exhibiting good antiradical and glutathione peroxidase-like activities. Up to a 14-fold increased activity was achieved compared with classical chemotherapeutic agents, exhibiting also different mechanisms of action (cell cycle assays). Redox analysis on HeLa cells suggested an increase of ROS levels after the incubation period.

CONCLUSION: the combination of organoselenium and phenolic moieties might provide valuable lead compounds with relevant antiproliferative properties.