Synthesis and antineoplastic activity of a novel series of phosphoramide mustard analogues of pyrimidine deoxyribonucleosides.
A novel series of cyclophosphamide derivatives of pyrimidine deoxyribonucleosides (6-9) has been synthesized from the corresponding amino nucleosides. Our preliminary findings have shown that three of these cyclophosphamide nucleoside analogues, 6, 7, and 9, have potent inhibitory effects on the replication of L1210 cells in vitro (ED50 = 1.2-1.5 x 10(-5) M). Since cyclophosphamide (cytoxan) has no cytotoxicity under these conditions, our findings indicate that these novel phosphamide derivatives have unusual biological properties which may include a unique mode of activation.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D002455:Cell Division / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D003853:Deoxyribonucleosides / Q000138:chemical synthesis* / Q000494:pharmacology; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D010752:Phosphoramide Mustards / Q000138:chemical synthesis* / Q000494:pharmacology; D011741:Pyrimidine Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D003853:Deoxyribonucleosides; D010752:Phosphoramide Mustards; D011741:Pyrimidine Nucleosides