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    • 89. 发明授权
    • 젤다나마이신 유도체, 이의 약학적으로 허용가능한 염,이의 제조방법 및 이를 유효성분으로 함유하는 암 예방 및치료제
    • 药物衍生物,其药物可接受的盐,其制备方法和用于预防和治疗含有其作为活性成分的肿瘤的药剂
    • KR100796637B1
    • 2008-01-22
    • KR1020060095804
    • 2006-09-29
    • 한국생명공학연구원
    • 홍영수이경이정준김영란김원철
    • C07D245/06A61K31/395
    • C07D225/02
    • Geldanamycin derivatives are provided to inhibit activity of hsp90(heat shock protein 90) as a chaperone associated with growth of cancer cells and metastasis, so that they are useful for prevention and treatment of tumor and degenerative neuronal disease. Geldanamycin derivatives for prevention and treatment of tumor are represented by the formula(1), wherein X is -OR1 or -NHR2 in which R1 is C1-5 alkyl and R2 is C1-C5 alkyl, C1-C5 alkenyl, mono- or di-alkylamino-C4-C5 alkylamino substituted by C1-C5 alkyl, halogen-substituted C1-C5 haloalkylamino or C1-C7 heterocycloalkyl-substituted C1-C5 alkylamino having at least one homologous or heterologous atom; and Y and Z are each independently hydrogen, -COR3 or -CONHR4 in which R3 is C1-C5 alkylcarbonyl-C1-C5 alkyl and R4 is hydrogen or C1-C5 alkyl.
    • 提供格尔德霉素衍生物以抑制hsp90(热休克蛋白90)作为与癌细胞和转移生长相关的分子伴侣的活性,从而可用于预防和治疗肿瘤和退行性神经元疾病。 用于预防和治疗肿瘤的格尔德霉素衍生物由式(1)表示,其中X是-OR1或-NHR2,其中R1是C1-5烷基,R2是C1-C5烷基,C1-C5链烯基,单或二 被C 1 -C 5烷基取代的 - 烷基氨基-C 4 -C 5烷基氨基,具有至少一个同源或异源原子的卤素取代的C 1 -C 5卤代烷基氨基或C 1 -C 7杂环烷基取代的C 1 -C 5烷基氨基; 并且Y和Z各自独立地为氢,-COR 3或-CONHR 4,其中R 3为C 1 -C 5烷基羰基-C 1 -C 5烷基,且R 4为氢或C 1 -C 5烷基。