Inhibition of nucleoside uptake into Ehrlich ascites carcinoma cells by new cytostatic methylhydrazones

Abstract

For the purpose of studying the structure-activity relationships of N'-methyl-N'-beta-chloroethylbenzaldehyde hydrazones, new hydrazones were synthesized in which the beta-chloroethyl group was replaced by substituents conveying a partial positive charge at the N' moiety by induction and/or mesomerism. In a preliminary antitumor evaluation, some of these hydrazones showed a cytostatic activity in vivo similar to that of the beta-chloroethyl hydrazones. The new hydrazones also strongly inhibit the uptake of nucleosides into tumor cells and intensify the in vivo cytostatic effect of methotrexate.