Discovery and synthesis of novel Wogonin derivatives with potent antitumor activity in vitro.
Discovery and synthesis of novel Wogonin derivatives with potent antitumor activity in vitro.
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DOI：
10.1016/j.ejmech.2017.09.046
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发表时间：
2017-11
影响因子：
6.7
通讯作者：
Jubo Wang;Raoling Ge;Xiaqiu Qiu;Xi Xu;Libin Wei;Zhiyu Li;Jinlei Bian
中科院分区：
文献类型：
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作者：
Jubo Wang;Raoling Ge;Xiaqiu Qiu;Xi Xu;Libin Wei;Zhiyu Li;Jinlei Bian
Phenotypic screening of high quality compound library is one of the most effective strategy to obtain novel bioactive compounds. Recently, our group have constructed a Wogonin-scaffold library with substituents diversity and successfully obtained a series of potent compounds. Herein, we reported the synthesis of these compounds and evaluated thein vitroantitumor activity against a panel of human tumor cell lines. Most of them showed good activity with a broad spectrum and preliminary structure-activity relationship for the substitutions were obtained. Further biological assays showed that the most potent compounds18nand20bcould significantly enhance the intracellular ROS level and induce the cell apoptosis at low micromole level. Through similarity searching, CDK9 was identified as the potential target for20b, which could be a start point for next structure-based drug design.
