Design, synthesis and anticancer activity evaluation of novel C14 heterocycle substituted epi-triptolide
Design, synthesis and anticancer activity evaluation of novel C14 heterocycle substituted epi-triptolide
复制标题
新型C14杂环取代表雷公藤甲素的设计、合成及抗癌活性评价
DOI：
10.1016/j.ejmech.2013.11.044
复制
发表时间：
2014-02-12
影响因子：
6.7
通讯作者：
Li, Yuanchao
中科院分区：
文献类型：
--
作者：
Xu, Hongtao;Tang, Huanyu;Li, Yuanchao
合成了两种新型C14杂环取代雷公藤甲素衍生物，并对SKOV-3和PC-3肿瘤细胞株进行了细胞毒性试验。在先导化合物上引入C14 -芳基杂环胺甲基取代基是一种有效的修饰方法，可以保留其有效的抗癌活性。同时，具有C14 -羟基的表riptolide衍生物系列（21-40）仍然保留了天然产物的细胞毒性。这显然挑战了雷公藤甲素的经典结构活性关系，认为C14 -羟基是其抗癌活性所必需的。(C) 2013 Elsevier Masson SAS。版权所有。
Two series of novel C14 heterocycle substituted epi-triptolide derivatives as potential anticancer agents were synthesized and tested for their cytotoxicity against SKOV-3 and PC-3 tumor cell lines. The introduction of C14 beta-aryl heterocycle aminomethyl substituent to the leading compound was found to be an effective modification method to retain the potent anticancer activity. Meanwhile, the series of epitriptolide derivatives (21-40) with C14 alpha-hydroxyl group, still retained the natural product's cytotoxicity. This is apparently challenges the classical structure activity relationship of triptolide that considers the C14 beta-hydroxyl group to be essential for its anticancer activity. (C) 2013 Elsevier Masson SAS. All rights reserved.