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    • 16. 发明授权
    • Maytansinoids, pharmaceutical compositions thereof and methods of use
thereof
    • 美登木素生物碱,其药物组合物及其使用方法
    • US4260608A
    • 1981-04-07
    • US92953
    • 1979-11-09
    • Osamu MiyashitaHiroshi Akimoto
    • Osamu MiyashitaHiroshi Akimoto
    • A61K31/535A61P35/00C07D498/18C07D498/16
    • C07D498/18
    • Novel maytansinoids of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, an alkyl group which may optionally be substituted or a group of the formula: --A.sup.1 --Y.sup.1 wherein A.sup.1 is an alkylene group or a bond, and Y.sup.1 is a cycloalkyl, phenyl, indolyl or imidazolyl group which may optionally be substituted,R.sup.2 is hydrogen atom, an alkyl, cycloalkyl or benzyl group,R.sup.3 is hydrogen atom, an alkyl group which may optionally be substituted, alkoxy, bornyloxy, isobornyloxy, benzyloxy group or a group of the formula: --A.sup.2 --Y.sup.2 wherein A.sup.2 is an alkylene group or a bond, and Y.sup.2 is an alicyclic hydrocarbon, phenyl or heterocyclic group which may optionally be substituted,provided that R.sup.3 is not an unsubstituted C.sub.1-4 alkyl group when both R.sup.1 and R.sup.2 are methyl groups, have antimicrobial antimitotic and antitumor activities.
    • 新型美登木素素,其分子式如下:其中R 1为氢原子,可任意取代的烷基或下式基团-A1-Y1其中A1为亚烷基或键,Y1为环烷基, 苯基,吲哚基或咪唑基,其可以任选被取代,R 2是氢原子,烷基,环烷基或苄基,R 3是氢原子,可任意被取代的烷基,烷氧基,苄氧基, 其中A2是亚烷基或键,Y2是可任选被取代的脂环烃,苯基或杂环基,条件是当R 3不是未取代的C 1-4烷基时, 和R2是甲基,具有抗微生物抗生素和抗肿瘤活性。