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  • Title: Searching phase II enzymes inducers, from Michael acceptor-[1,2]dithiolethione hybrids, as cancer chemopreventive agents.
    Author: Couto M, de Ovalle S, Cabrera M, Cerecetto H, González M.
    Journal: Future Med Chem; 2015; 7(7):857-71. PubMed ID: 26061105.
    Abstract:
    BACKGROUND: Cancer chemoprevention involves the carcinogenic process prevention, delay or reverse by the administration of chemopreventive agents, which are able to suppress or block the carcinogen metabolic activation/formation. The increased activity of phase II detoxification enzymes such as quinone-reductase (QR) and glutation-S-transferase (GST) correlates with the protection against chemically-induced carcinogenesis. It has been shown that synthetic chalcones and 3H-[1,2]-dithiole-3-thiones promote expression of genes involved in chemoprevention. MATERIALS & METHODS: Herein, the induction of phase II enzymes by designed Michael acceptor-dithiolethione hybrids was studied. RESULTS & DISCUSSION: Hybrids 5 and 7 displayed the induction of quinone-reductase and glutation-S-transferase in vitro in the same order on the wild-type mouse-hepatoma Hepa 1c1c7 and on the aryl-hydrocarbon-nuclear-translocator (Arnt)-defective mutant BPrc1 cells indicating that 7 displays the best chemopreventive potential.
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