Article ID Journal Published Year Pages File Type
1397182 European Journal of Medicinal Chemistry 2006 4 Pages PDF
Abstract

Chemoprevention can be defined as an intervention in the carcinogenic process by use of natural or synthetic substances. Induction of Phase II enzyme is an important mechanism of chemoprevention. In the present studies we have synthesized several derivatives of (+)(–) 4-methylsulfinyl-1-(S-methyldithiocarbamyl)-butane (sulforamate) and evaluated their effectiveness as monofunctional inducer of the NAD(P)H Quinone oxidoreductase [quinone reductase (QR)] a phase II enzyme in cultured Hepa1c1c7 murine hepatoma cells. The cytotoxicity of some of the derivatives was strongly reduced in comparison to [(–)-1-isothiocyanato-4(R)-(methylsulfinyl)butane] (sulforaphane). However, the induction potential of these compounds was comparable to sulforaphane. On the basis of these results sulforamate derivatives can be regarded as simple, inexpensive and readily available chemopreventive agents.

Graphical abstractSynthesis of several derivatives of (+)(-) 4-methylsulfinyl-1-(S-methyldithio-carbamyl)butane (sulforamate) and their evaluation as monofunctional inducer of NAD(P)HQuinone oxidoreducatse[quinone reductase (QR)] was carried out.Figure optionsDownload full-size imageDownload as PowerPoint slide

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