Isolation, purification, synthesis, and antiinvasive/antimetastatic activity of U-77863 and U-77864 from Streptomyces griseoluteus, strain WS6724.
In screening of actinomycetes for structures with differential solid tumor activity, Streptomyces griseoluteus, strain WS6724 was found to produce U-77863 and U-77864. U-77863 exhibited antiinvasive activity in vitro in the membrane invasion culture system (MICS) and a dose-dependent antimetastatic activity in vivo versus K1735-M2 and B16-F10 murine melanomas. The isolation, purification, and synthesis of both structures and biological activity is reported.
Harper
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Upjohn Laboratories, Kalamazoo, Michigan 49001.
Welch
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D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000302:isolation & purification* / Q000494:pharmacology*; D002934:Cinnamates / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D008175:Lung Neoplasms / Q000188:drug therapy; D008546:Melanoma, Experimental / Q000188:drug therapy; D051379:Mice; D008809:Mice, Inbred C3H; D008810:Mice, Inbred C57BL; D009361:Neoplasm Invasiveness; D009362:Neoplasm Metastasis; D010666:Phenylpropionates / Q000138:chemical synthesis / Q000302:isolation & purification* / Q000494:pharmacology; D013302:Streptomyces / Q000737:chemistry* / Q000145:classification; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D002934:Cinnamates; D010666:Phenylpropionates; C079457:trans-3-(2'-methylphenyl)-2-propene-1-carboxamide; C079458:U 77864