Design, synthesis, and evaluation of a radicicol and geldanamycin chimera, radamide
Design, synthesis, and evaluation of a radicicol and geldanamycin chimera, radamide
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DOI：
10.1021/ol048266o
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发表时间：
2004-11-25
期刊：
影响因子：
5.2
通讯作者：
Blagg, BSJ
中科院分区：
文献类型：
--
作者：
Clevenger, RC;Blagg, BSJ
天然产物根赤霉素和格尔德霉素通过酰胺键将根赤霉素的间苯二酚部分连接到格尔德霉素的醌环上，制备了一种由根赤霉素和格尔德霉素组成的嵌合体。这些化合物的抑制活性通过它们抑制Hsp 90固有的ATP酶活性的能力来确定，沿着MCF-7乳腺癌细胞中Hsp 90客户蛋白HER-2的降解。
A chimera composed of the natural products radicicol and geldanamycin has been prepared through an amide linkage connecting the resorcinol moiety of radicicol to the quinone ring of geldanamycin. The inhibitory activity of these compounds was determined by their ability to inhibit Hsp90's inherent ATPase activity along with degradation of the Hsp90 client protein, HER-2 in MCF-7 breast cancer cells.