Antitumor activity of novel deoxoartemisinin monomers, dimers, and trimer
Antitumor activity of novel deoxoartemisinin monomers, dimers, and trimer
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DOI：
10.1021/jm020119d
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发表时间：
2003-03-13
影响因子：
7.3
通讯作者：
Kim, SK
中科院分区：
文献类型：
--
作者：
Jung, M;Lee, S;Kim, SK
具有C-12非缩醛官能团的脱氧青蒿素的第一伯胺9和溴烷基类似物7被制备为合成各种衍生物的多种中间体。用新的化学方法合成了8个C-12非缩醛二聚体和1个脱氧青蒿素三聚体。二聚体，特别是12a、18a、b和三聚体17，在抑制某些人类癌细胞株的生长方面特别有效和选择性，与临床使用的抗癌药物相当。具有一个酰胺或一个硫中心的二聚体的两个乙烯基团的连接基对于高抗癌活性是必不可少的。Trimer 17对测试的大多数人类癌细胞株显示出非常强的活性。
The first primary amines 9 and bromoalkyl analogues 7 of deoxoartemisinin with nonacetal functionality at C-12 are prepared as versatile intermediates for the synthesis of various derivatives. Eight C-12 nonacetal type dimers and one trimer of deoxoartemisinin were prepared using novel chemistry. Dimers, particularly 12a, 18a,b, and trimer 17, were especially potent and selective at inhibiting the growth of certain human cancer cell lines and were comparable to that of clinically used anticancer drugs. The linker with one amide- or one sulfur-centered two ethylene groups of the dimers is essential for high anticancer activity. Trimer 17 shows very potent activity against most of the human cancer cell lines tested.