Synthesis and evaluation of novel alkannin and shikonin oxime derivatives as potent antitumor agents.
Synthesis and evaluation of novel alkannin and shikonin oxime derivatives as potent antitumor agents.
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DOI：
10.1016/j.bmcl.2014.07.012
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发表时间：
2014-09
影响因子：
2.7
通讯作者：
Rubing Wang;Xu Zhang;Hualong Song;Shanshan Zhou;Shaoshun Li
中科院分区：
文献类型：
--
作者：
Rubing Wang;Xu Zhang;Hualong Song;Shanshan Zhou;Shaoshun Li
首次设计合成了40个紫草素和紫草素肟衍生物。测定了它们对三种肿瘤细胞和正常细胞的细胞毒作用，并与紫草素和紫草素进行了比较。基于细胞的研究表明，一些肟衍生物对先导化合物具有更好的或相对有效的作用，特别是它们对K562细胞的选择性和优异的抗肿瘤活性，对正常细胞没有毒性。因此，对紫草素和紫草素的母核进行肟化修饰是获得有效抗肿瘤药物的有效途径。
A set of forty alkannin and shikonin oxime derivatives were firstly designed and synthesized. Their cytotoxicities against three kinds of tumor cells and a normal cell line were tested and compared with alkannin and shikonin. The cell-based investigation demonstrated that some oxime derivatives were more or comparatively effective to the lead compounds, especially their selective and excellent antitumor activities towards K562 cells with no toxicity in normal cells. We may conclude that oximate modification to the mother nucleus of alkannin and shikonin is an available approach to acquire potent antitumor agents.