Cancer chemopreventive activity of sulforamate derivatives

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.

Synthesis 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 as PowerPoint slide