stubomycin and Sarcoma-180

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.

Topics: Animals; Antibiotics, Antineoplastic; Bacteria; Carbonates; Female; HeLa Cells; Mice; Mice, Inbred ICR; Microbial Sensitivity Tests; Molecular Structure; Polyenes; Sarcoma 180; Structure-Activity Relationship

Amino acyl derivatives of hitachimycin have been synthesized and evaluated their activities including antibacterial, cytocidal against HeLa cells and in vivo antitumor against sarcoma 180. 15-O-(tert-Butoxycarbonyl(BOC)-glycyl)hitachimycin (2), 15-O-(BOC-beta-alanyl)hitachimycin (4), 15-O-(BOC-(O-tert-Bu)-glutamyl)hitachimycin (6) and 15-O-L-alanylhitachimycin (11) showed comparable in vivo antitumor activity with hitachimycin and the solubility of these compounds was improved.

Topics: Animals; Antibiotics, Antineoplastic; Bacteria; Chemical Phenomena; Chemistry; Chromatography, High Pressure Liquid; HeLa Cells; Humans; Magnetic Resonance Spectroscopy; Molecular Structure; Polyenes; Sarcoma 180; Solubility; Tumor Cells, Cultured

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.

Topics: Acylation; Animals; Anti-Bacterial Agents; Antibiotics, Antineoplastic; Cell Survival; Chemistry, Pharmaceutical; Drug Screening Assays, Antitumor; HeLa Cells; Humans; Lactams; Magnetic Resonance Spectroscopy; Mice; Mice, Inbred ICR; Polyenes; Sarcoma 180

The antitumor activity of a new antibiotic, stubomycin, against various murine tumors was studied. Stubomycin showed antitumor activity against Sarcoma 180, IMC-carcinoma and Meth-A tumor. In particular, all of the mice inoculated i.p. with IMC-carcinoma were cured when they were given nine successive injections of stubomycin. Stubomycin also showed remarkable antitumor effects against Sarcoma 180 and Ehrlich ascites carcinoma when administered concomitantly with bleomycin.

Topics: Animals; Antibiotics, Antineoplastic; Carcinoma, Ehrlich Tumor; Male; Mice; Mice, Inbred Strains; Neoplasms, Experimental; Polyenes; Sarcoma 180