Chemical modification of hitachimycin. II. Synthesis and antitumor activities of carbonate derivatives.

Abstract

Several carbonate derivatives of hitachimycin have been synthesized and evaluated their activities including antibacterial, cytocidal against HeLa cells and in vivo antitumor against Sarcoma 180. Some of these derivatives showed higher antitumor activity than hitachimycin. Among the derivatives, 11,15-di-O-methoxycarbonylhitachimycin (2), 11,15-di-O-ethoxycarbonylhitachimycin (3) and 15-O-methoxycarbonylhitachimycin (9) were most effective in in vivo assay.

• Authors: K Shibata, S Satsumabayashi, H Sano, K Komiyama, Z B Yang, A Nakagawa, S Omura
• Journal: The Journal of antibiotics (J Antibiot (Tokyo)) Vol. 42 Issue 5 Pg. 718-26 (May 1989) ISSN: 0021-8820 [Print] England
• PMID: 2722686 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antibiotics, Antineoplastic
• Carbonates
• Polyenes
• stubomycin

Topics

• Animals
• Antibiotics, Antineoplastic
• Bacteria (drug effects)
• Carbonates (chemical synthesis, pharmacology, therapeutic use)
• Female
• HeLa Cells (drug effects)
• Mice
• Mice, Inbred ICR
• Microbial Sensitivity Tests
• Molecular Structure
• Polyenes (chemical synthesis, pharmacology, therapeutic use)
• Sarcoma 180 (drug therapy)
• Structure-Activity Relationship