Synthesis and antitumor activity of cis-dichloroplatinum (II)-N-aminated nucleoside complexes.
N-Aminated nucleoside complexes of cis-dichloroplatinum(II) were synthesized, and their antitumor activities against L1210 cells in mice and in vitro were studied. While the native nucleosides failed to show any antitumor activity, the complexes exhibited high antitumor activity and had no nephrotoxicity in mice. Studies on their mode of action in vitro indicated that the ligands played characteristic roles in the appearance of antitumor activity; ribonucleoside complexes caused the inhibition of RNA synthesis, and deoxyribo- or arabinonucleoside complexes caused the inhibition of DNA synthesis.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002945:Cisplatin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use / Q000633:toxicity; D004261:DNA Replication / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D007202:Indicators and Reagents; D007668:Kidney / Q000187:drug effects; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D008813:Mice, Inbred ICR; D009705:Nucleosides / Q000138:chemical synthesis* / Q000627:therapeutic use / Q000633:toxicity; D014176:Protein Biosynthesis / Q000187:drug effects; D013329:Structure-Activity Relationship; D014158:Transcription, Genetic / Q000187:drug effects
D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D009705:Nucleosides; D002945:Cisplatin