Chemical modification of hitachimycin. Synthesis, antibacterial, cytocidal and in vivo antitumor activities of hitachimycin derivatives.
Several acyl derivatives of hitachimycin have been synthesized and their activities, including antibacterial, cytocidal against HeLa cells and in vivo antitumor against sarcoma 180, evaluated. Some of these derivatives showed higher antitumor activity than hitachimycin. Among the derivatives, 11-O-propionyl-15-O-butyrylhitachimycin (12) and the 11-O-acylhitachimycins (15-17) were most effective in in vivo assay.
Shibata
K
K
Nippon Dental University, Tokyo, Japan.
Satsumabayashi
S
S
Sano
H
H
Komiyama
K
K
Nakagawa
A
A
Omura
S
S
D000215:Acylation; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis*; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis*; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D007769:Lactams; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008813:Mice, Inbred ICR; D011090:Polyenes / Q000138:chemical synthesis / Q000494:pharmacology; D012510:Sarcoma 180 / Q000188:drug therapy
D000900:Anti-Bacterial Agents; D000903:Antibiotics, Antineoplastic; D007769:Lactams; D011090:Polyenes; C031780:stubomycin