SYNTHESIS, DNA INTERACTION AND ANTINEOPLASTIC ACTIVITY OF SEMICARBAZONE DERIVATIVES

A number of antineoplastic agents including procarbazine and bisantren e derive from hydrazine, but so far none have been developed from semi carbazide. In order to assay active minimal structures, thirteen new c ompounds were prepared by replacing hydrogen atoms in semicarbazone am ine group by alkylamine moieties, employing an improved procedure. DNA binding was evaluated by treatment of a drug solution with DNA-cellul ose complex and further measurement of remaining drug by UV spectrosco py and the affinity observed to range from medium to weak. On testing these compounds against human neoplastic cell lines, only a nitroderiv ative proved active on CNS and Breast cell lines at 10(-4) M. This mem ber was studied by cyclic voltammetry.