Inhibition of nucleoside uptake into Ehrlich ascites carcinoma cells by new cytostatic methylhydrazones.
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.
D000818:Animals; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy* / Q000378:metabolism; D002455:Cell Division / Q000187:drug effects; D004273:DNA, Neoplasm / Q000096:biosynthesis; D004357:Drug Synergism; D006019:Glycolysis / Q000187:drug effects; D006835:Hydrazones / Q000494:pharmacology*; D008297:Male; D008727:Methotrexate / Q000494:pharmacology; D051379:Mice; D009705:Nucleosides / Q000378:metabolism*; D012334:RNA, Neoplasm / Q000096:biosynthesis; D013329:Structure-Activity Relationship
D004273:DNA, Neoplasm; D006835:Hydrazones; D009705:Nucleosides; D012334:RNA, Neoplasm; D008727:Methotrexate