title: Chemical modification of hitachimycin. III. Synthesis and antitumor activities of amino acyl derivatives.
abstract: 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.
authors.affiliation: Nippon Dental University, Tokyo, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Shibata
authors.forename: S
authors.initials: S
authors.lastname: Satsumabayashi
authors.forename: H
authors.initials: H
authors.lastname: Sano
authors.forename: K
authors.initials: K
authors.lastname: Komiyama
authors.forename: Z B
authors.initials: ZB
authors.lastname: Yang
authors.forename: A
authors.initials: A
authors.lastname: Nakagawa
authors.forename: S
authors.initials: S
authors.lastname: Omura
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects*; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D011090:Polyenes / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D012510:Sarcoma 180 / Q000188:drug therapy*; D012995:Solubility; D014407:Tumor Cells, Cultured
chemical_list: D000903:Antibiotics, Antineoplastic; D011090:Polyenes; C031780:stubomycin