[Design, synthesis and antiproliferative activity in cancer cells of novel dihydropyrazolyl and pyrazolyl artemisinin-phenyl ethers]

Yun-Fei Wei; Min Huang; Ai-Hua Li; Feng Zhao; Hang Zhong; Dan Liu; Lin-Xiang Zhao

doi:10.19540/j.cnki.cjcmm.20180613.002

[Design, synthesis and antiproliferative activity in cancer cells of novel dihydropyrazolyl and pyrazolyl artemisinin-phenyl ethers]

Zhongguo Zhong Yao Za Zhi. 2018 Sep;43(17):3582-3588. doi: 10.19540/j.cnki.cjcmm.20180613.002.

[Article in Chinese]

Authors

Yun-Fei Wei¹, Min Huang¹, Ai-Hua Li¹, Feng Zhao¹, Hang Zhong¹, Dan Liu¹, Lin-Xiang Zhao¹

Affiliation

¹ Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China.

PMID: 30347929
DOI: 10.19540/j.cnki.cjcmm.20180613.002

Abstract

To explore potent anticancer agent based on artemisinin scaffold, a series of 10-O-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.

Keywords: artemisinin; cancer therapy; natural product modifications; ntiproliferation.

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology*
Artemisinins / chemistry*
Cell Line, Tumor
Cell Proliferation
Drug Design
Drug Screening Assays, Antitumor
Humans
Phenyl Ethers / chemical synthesis*
Phenyl Ethers / pharmacology*
Structure-Activity Relationship

Substances

Antineoplastic Agents
Artemisinins
Phenyl Ethers