Improved synthesis and antitumor activity of 2-bromo-2'-deoxyadenosine.

Abstract

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.

• Authors: M C Huang, T L Avery, R L Blakley, J A Secrist 3rd, J A Montgomery
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 27 Issue 6 Pg. 800-2 (Jun 1984) ISSN: 0022-2623 [Print] United States
• PMID: 6610764 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Antineoplastic Agents
• Deoxyadenosines
• 2'-bromo-2'-deoxyadenosine

Topics

• Animals
• Antineoplastic Agents (chemical synthesis)
• Deoxyadenosines (analogs & derivatives, chemical synthesis, therapeutic use)
• Female
• Leukemia L1210 (drug therapy)
• Melanoma (drug therapy)
• Mice
• Ovarian Neoplasms (drug therapy)