Design, synthesis and antiproliferative activity in cancer cells of novel dihydropyrazolyl and pyrazolyl artemisinin-phenyl ethers.
10.19540/j.cnki.cjcmm.20180613.002
- Author:
Yun-Fei WEI
1
;
Min HUANG
1
;
Ai-Hua LI
1
;
Feng ZHAO
1
;
Hang ZHONG
1
;
Dan LIU
1
;
Lin-Xiang ZHAO
1
Author Information
1. Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China.
- Publication Type:Journal Article
- Keywords:
artemisinin;
cancer therapy;
natural product modifications;
ntiproliferation
- From:
China Journal of Chinese Materia Medica
2018;43(17):3582-3588
- CountryChina
- Language:Chinese
-
Abstract:
To explore potent anticancer agent based on artemisinin scaffold, a series of 10--phenyl ethers derivatives containing dihydropyrazolyl or pyrazolyl moiety have been designed and synthesized. Their structures were determined by LC-MS and ¹H-NMR date. Inhibitory effects of the target compounds in human breast cancer MCF-7, MCF/Adr, MDA-MB-231 cells and prostate cell line PC-3 were determined by MTT assay. Those derivatives displayed good antiproliferative activity against the tested cancer cells. Particularly, target compounds exhibited significant cytotoxicity against drug-resistance cells MCF/Adr, which was worthy for further investigation.
