首页> 外国专利> THE GLYCOSYLATED NON-QUINONE GELDANAMYCIN DERIVATIVES HAVING INCREASED SOLUBILITY OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION FOR HEAT SHOCK PROTEIN(HSP90) ATPASE INHIBITOR CONTAINING SAME

THE GLYCOSYLATED NON-QUINONE GELDANAMYCIN DERIVATIVES HAVING INCREASED SOLUBILITY OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COMPOSITION FOR HEAT SHOCK PROTEIN(HSP90) ATPASE INHIBITOR CONTAINING SAME

机译:糖基化非醌型格尔德霉素衍生物具有增加的溶解度或药学上可接受的盐的含量,其制备方法和组成包含热休克蛋白(HSP90)ATPase抑制剂的药物组成

摘要

PURPOSE: A glycosylated non-quinone geldanamycin derivative with enhanced solubility or a pharmaceutically acceptable salt thereof and a pharmaceutical composition for suppressing HSP90 ATPase activity are provided to prevent or treat cancer. CONSTITUTION: A glycosylated non-quinone geldanamycin derivative or a pharmaceutically acceptable salt thereof contains a compound of chemical formulas 1-5. The derivative enhances solubility and suppresses HSP ATPase activity. The derivative is prepared by transglycosylation using isolated glycosyltransferase and a non-quinone geldanamycin derivative. The glycosyltransferase is UDP-glycosyltransferase derived from Bacillus licheniformis.
机译:用途:提供了具有增强的溶解度的糖基化非醌格尔德霉素衍生物或其药学上可接受的盐,以及用于抑制HSP90 ATPase活性的药物组合物,以预防或治疗癌症。组成:糖基化的非醌格尔德霉素衍生物或其药学上可接受的盐含有化学式1-5的化合物。该衍生物增强溶解度并抑制HSP ATPase活性。使用分离的糖基转移酶和非醌格尔德霉素衍生物通过转糖基化制备衍生物。糖基转移酶是衍生自地衣芽孢杆菌的UDP-糖基转移酶。

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