Synthesis and evaluation of 8,9-amido analogs of geldanamycin
Synthesis and evaluation of 8,9-amido analogs of geldanamycin
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DOI：
10.1016/j.tetlet.2009.09.091
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发表时间：
2009-12-02
影响因子：
1.8
通讯作者：
Neckers, Leonard M.
中科院分区：
文献类型：
--
作者：
Andrus, Merritt B.;Wong, Yong;Neckers, Leonard M.
设计、合成了抗癌药物格尔达那霉素的氨基类似物，并用SKBR3细胞进行了检测，其中HER2受体酪氨酸激酶的稳定性依赖于伴侣Hsp90。在C8，9位使用酰胺作为三取代烯烃异构体，通过两个主要片段，即苯胺-胺左侧部分和二元酸右侧部分，提供了一种简化的聚合合成方法。(C)2009爱思唯尔有限公司。保留所有权利。
Amido analogs of geldanamycin, an ansamycin anticancer agent, were designed, synthesized, and assayed with SKBR3 cells, in which stability of HER2 receptor tyrosine kinase is dependent on the chaperone Hsp90. An amide was employed as a trisubstituted alkene isostere at the C8,9 position, which provided for a simplified, convergent synthesis through two major fragments, an aniline-amine left-hand portion and a dicarboxylic acid right-hand piece. (C) 2009 Elsevier Ltd. All rights reserved.