Chinese Academy of Medical Sciences

The Second Affiliated Hospital of Guangzhou University of Chinese Medicine

Guangdong Provincial Hospital of Tcm

The Second Clinical College of Guangzhou University of Chinese Medicine

Ennian Li

Bo Liu

Kai Wang

Xiaodong Han

Yi Wang

Yiqi Yang

Yunshan Wu

Liqiao Han

Hualun Liang

Xiaowan Wang

Xianzhang Huang

Runyue Huang

Bidan Zheng

Zhimin Yang

Jinlang Zhong

Quanfu Chen

Disclosed in the present invention is a new triptolide derivative as shown in formula (I). Also disclosed in the present invention are a preparation method for the compound and the medical use thereof in preparation of anti-cancer drugs. Triptolide acrylate of the present invention and a pharmaceutically acceptable salt thereof have anti-cancer activity, and after animal in-vivo experiments, can effectively inhibit tumor growth in animals. A plurality of in-vitro experiments proves that same can significantly increase the protein expression quantity of p53, promote the apoptosis of tumor cells, effectively inhibit the growth of the tumor cells, and have the effect of inhibiting metastasis of cancer cells. More importantly, the toxicity of the compound to normal cells is less than that of triptolide. 

Triptolide acrylate, preparation method therefor and use thereof

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Guangdong, China

Ennian Li