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1. (WO2018196581) DIHYDROARTEMISININ-STEROID CONJUGATE AND PREPARATION METHOD AND USE THEREOF

Pub. No.:    WO/2018/196581    International Application No.:    PCT/CN2018/082120
Publication Date: Fri Nov 02 00:59:59 CET 2018 International Filing Date: Mon Apr 09 01:59:59 CEST 2018
IPC: C07J 17/00
A61K 31/56
A61P 35/00
Applicants: SHEN, Zhengwu
沈征武
Inventors: SHEN, Zhengwu
沈征武
ZHANG, Jinghua
张菁华
Title: DIHYDROARTEMISININ-STEROID CONJUGATE AND PREPARATION METHOD AND USE THEREOF
Abstract:
Disclosed is a dihydroartemisinin-steroid conjugate having the following general formula (I) or a pharmaceutically acceptable salt thereof, wherein the dihydroartemisinin molecule at the position 10 thereof is connected to the parent nucleus of the steroid through a linker X. Also disclosed in the present invention are a method for preparing the dihydroartemisinin-steroid conjugate and the use of the same in the preparation of a drug for treating cancers. The dihydroartemisinin-steroid conjugate of the present invention shows a very strong inhibitory activity on multiple tumour cell lines, has small toxicity, can penetrate the blood brain barrier and has very broad application prospects.