Convenient syntheses of novel 1-isothiocyano-alkylphosphonate diphenyl ester derivatives with potential biological activity

Herein, we describe a convenient method for the syntheses of novel 1-isothiocyano-alkylphosphonate diaryl ester derivatives and their antiproliferative activity. The syntheses are based on dithiocarbamates obtained in situ with the use of carbon disulfide under basic conditions, and their desulfurization using several different reagents, of which hydrogen peroxide proved to be the most efficient. The compounds synthesized demonstrated high antiproliferative activity against several cancer cell lines in vitro, and also showed some activity as serine protease inhibitors.