Synthesis of 1-beta-D-ribofuranosyl-1,2-dihydropyrimidin-2-one derivatives and their biological activities.
Several alkyl substituted 1-beta-D-ribofuranosyl-1,2-dihydropyrimidin-2-one derivatives were synthesized by the method of stannic chloride-catalyzed glycosidation method to elucidate their inhibitory activity of cytidine deaminase and also their antitumor activities in vitro and in vivo. Alkyl substitution at position 4 or 6 of the derivatives decreased their inhibitory activity for cytidine deaminase and also decreased antitumor activity against L1210 cells in vitro.
D000818:Animals; D003564:Cytidine Deaminase / Q000037:antagonists & inhibitors*; D004353:Drug Evaluation, Preclinical; D007202:Indicators and Reagents; D007700:Kinetics; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D009700:Nucleoside Deaminases / Q000037:antagonists & inhibitors*; D011741:Pyrimidine Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D007202:Indicators and Reagents; D011741:Pyrimidine Nucleosides; D009700:Nucleoside Deaminases; D003564:Cytidine Deaminase