Structure-activity relationship study on 13-deoxytedanolide, a highly antitumor macrolide from the marine sponge Mycale adhaerens
Structure-activity relationship study on 13-deoxytedanolide, a highly antitumor macrolide from the marine sponge Mycale adhaerens
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DOI：
10.1016/j.bmc.2004.10.014
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发表时间：
2005-01-17
影响因子：
3.5
通讯作者：
Fusetani, N
中科院分区：
文献类型：
--
作者：
Nishimura, S;Matsunaga, S;Fusetani, N
为了获得13-脱氧替丹酮的结构-活性关系（SAR）的信息，已经进行了化学转化，目标是这样的官能团，如环氧化物，羟基，酮和烯烃。共制备了10个衍生物，它们对P388小鼠白血病细胞的细胞毒性和酵母细胞裂解物中多肽延伸的抑制活性提供了一些重要的SAR;南半球包含药效团，而环氧化物侧链是必不可少的活性。(C)2004爱思唯尔有限公司保留所有权利。
To obtain information of structure-activity relationships (SARs) of 13-deoxytedanolide, its chemical transformation has been carried out, targeting on such functional groups as an epoxide, hydroxyls, ketones, and olefins. A total of 10 derivatives have been prepared and their cytotoxicity against P388 murine leukemia cells and inhibitory activity of polypeptide elongation in yeast cell lysate provided some important SARs; the southern hemisphere comprises the pharmacophore, while the epoxide-bearing side chain is essential for the activity. (C) 2004 Elsevier Ltd. All rights reserved.