Synthesis of some benzothiazole derivatives as possible alkylating agents

The title compounds 2-[2-(bis-(2-chloroethyl) amino)-methyl]-benzothiazoles (III) were synthesized by the reactions of corresponding 2-[2-(bis-(2-hydroxyethyl) amino) methyl] benzothiazole (IIA-D) with phosphorus trichloride and phosphorus oxychloride. The intermediates 2-chloromethyl benzothiazole derivatives (IA-D) and 2-[2-(bis-(2-hydroxyethyl) amino) methyl]-benzothiazole (IIA-D) were prepared by standard procedures. All the intermediates and title compounds were characterized by physical, chemical, analytical and spectral data. The biological evaluation of the compounds was carried out by various methods such as short term invitro cytotoxic activity and invivo anticancer screening. Compounds IIIB and IIIC showed significant anticancer activity.