Title:
DIHYDROARTEMISININ-STEROID CONJUGATE AND PREPARATION METHOD AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2018/196581
Kind Code:
A1
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.
Inventors:
SHEN ZHENGWU (CN)
ZHANG JINGHUA (CN)
ZHANG JINGHUA (CN)
Application Number:
PCT/CN2018/082120
Publication Date:
November 01, 2018
Filing Date:
April 08, 2018
Export Citation:
Assignee:
SHEN ZHENGWU (CN)
International Classes:
C07J17/00; A61K31/56; A61P35/00
Other References:
ANTONIOS S. LETIS ET AL.: "Synthesis and Cytotoxic Activity of New Artemisinin Hybrid Molecules Against Human Leukemia Cells", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 25, no. 13, 20 April 2017 (2017-04-20), pages 3357 - 3367, XP085037279
CINDY HORWEDEL ET AL.: "Cytotoxicity of Artesunic Acid Homo-and Heterodimer Molecules toward Sensitive and Multidrug-Resistant CCRF-CEM Leukemia Cells", J. MED. CHEM., vol. 53, no. 13, 31 December 2010 (2010-12-31), pages 4832 - 4848, XP055527505
See also references of EP 3617218A4
CINDY HORWEDEL ET AL.: "Cytotoxicity of Artesunic Acid Homo-and Heterodimer Molecules toward Sensitive and Multidrug-Resistant CCRF-CEM Leukemia Cells", J. MED. CHEM., vol. 53, no. 13, 31 December 2010 (2010-12-31), pages 4832 - 4848, XP055527505
See also references of EP 3617218A4
Attorney, Agent or Firm:
SHULUN & PARTNERS (SHANGHAI) (CN)
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