Improved synthesis and antitumor activity of 2-bromo-2'-deoxyadenosine.
A more convenient synthetic route to 2-bromo-2'-deoxyadenosine (5) is reported, and results indicating significant antitumor activity of 5 against three murine tumors (L1210 leukemia, B16 melanoma, and M5076 ovarian carcinoma) are presented. The antitumor activity is very schedule dependent, being much greater when the drug is given q 3 h (X8) every 3rd or 4th day than when given by single daily administration. Toxicity of 5 for the tumor-bearing host is also very schedule dependent. Thus, on the q 3 h schedule of administration, a greater cumulative dose is tolerated by the host, and the therapeutic effectiveness of 5 is enhanced accordingly.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis*; D003839:Deoxyadenosines / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use; D005260:Female; D007939:Leukemia L1210 / Q000188:drug therapy; D008545:Melanoma / Q000188:drug therapy; D051379:Mice; D010051:Ovarian Neoplasms / Q000188:drug therapy
D000970:Antineoplastic Agents; D003839:Deoxyadenosines; C036855:2'-bromo-2'-deoxyadenosine