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    • 5. 发明授权
    • Rhizoxin derivatives and their use as anti-tumor agents
    • 根瘤菌素衍生物及其作为抗肿瘤剂的用途
    • US5391564A
    • 1995-02-21
    • US195574
    • 1994-02-14
    • Masakatsu KanekoMakoto KamokariTomowo KobayashiKazuhiko Sasagawa
    • Masakatsu KanekoMakoto KamokariTomowo KobayashiKazuhiko Sasagawa
    • C07D493/22A61K31/365A61K31/675A61P35/00C07D493/18C07F9/6561
    • C07D493/18Y02P20/55
    • Rhizoxin and rhizoxin-2-ene derivatives of formula (I): ##STR1## in which: n is 1 to 25: A is an extra bond or oxygen, X is oxygen, sulfur, nitrogen or carbonyl; and R is hydrogen, carboxylic acyl having from 1 to 25 carbon atoms, alkoxycarbonyl group having from 2 to 26 carbon atoms, phosphono, alkylphosphono group in which the alkyl part has from 1 to 25 carbon atoms, dialkylphosphono group in which each alkyl part has from 1 to 25 carbon atoms, alkyl group having from 1 to 25 carbon atoms, aralkyl, cycloalkyl, heterocyclic, alkylthio group in which the alkyl part has from 1 to 25 carbon atoms, aralkylthio, or heterocyclylthio, or when X represents a nitrogen atom, R is R.sup.1 and R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, acyl, alkoxycarbonyl, phosphono, alkylphosphono or dialkylphosphono have valuable anti-tumor activity. They may be prepared by acylation of rhizoxin or rhizoxin-2-ene.
    • (I)的根瘤菌素和根瘤素-2-烯衍生物:其中:n为1至25:A为额外键或氧,X为氧,硫,氮或羰基; R为氢,具有1至25个碳原子的羧酰基,具有2至26个碳原子的烷氧基羰基,膦酰基,烷基部分为1至25个碳原子的烷基膦酰基,其中每个烷基部分具有的二烷基膦酰基 1至25个碳原子,具有1至25个碳原子的烷基,其中烷基部分具有1至25个碳原子的芳烷基,环烷基,杂环,烷硫基,芳烷硫基或杂环硫基,或当X表示氮原子时 R为R 1和R 2,其中R 1和R 2为氢,烷基,酰基,烷氧基羰基,膦酰基,烷基膦酰基或二烷基膦酰基具有有价值的抗肿瘤活性。 它们可以通过根瘤菌素或根瘤素-2-烯的酰化来制备。