Cytotoxic compounds. Part VIII. Some S-α-(acylamino)acyl-p-[di-(2-halogenoethyl)amino]thiophenols

Abstract

Fourteen thiolesters of this type have been synthesised by acylation of p-[di-(2-chloroethyl)amino]thiophenol, or the dibromo-analogue, with a variety of α-N-acylamino-acids in the presence of dicyclohexylcarbodi-imide. The deactivation of the “mustard” caused by this acylation of the thiol group, as measured by the diminished rate of hydrolysis of the halide, is similar to that brought about by simple acetylation.