INHIBITION OF NUCLEOSIDE UPTAKE INTO EHRLICH ASCITES-CARCINOMA CELLS BY NEW CYTOSTATIC METHYLHYDRAZONES

Google Scholar
  • 1 January 1978
    • journal article
    • research article
    • Vol. 38  (10) , 3512-3517
Abstract
The structure-activity relationships of N''-methyl-N''-.beta.-chloroethylbenzaldehyde hydrazones were studied. 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 hydrazones showed a cytostatic activity in vivo similar to that of the .beta.-chloroethyl hydrazones. The new hydrazones also strongly inhibited the uptake of nucleosides into tumor cells and intensified the in vivo cytostatic effect of methotrexate.