title: Design, synthesis and antitumor activity of novel artemisinin derivatives using hybrid approach.
abstract: In an attempt to develop potent and selective anti-tumor agents, two novel series of artemisinin-chalcone hybrids were designed, synthesized and screened for their antitumor activities against HT-29, A549, MDA-MB-231, HeLa and H460 cell lines in vitro. Nearly all of the tested compounds showed significantly increased anti-tumor activity compared with the corresponding dihydroartemisinin (DHA). Most of the title compounds displayed good selectivity toward HT-29 and HeLa cell lines with IC₅₀ values ranging from 0.09 to 0.85 µM. Among them, the most promising compound 9c (IC₅₀) range of 0.09-0.93 µM) was 10.5- to 70-times more active than DHA (IC₅₀ range of 5.6-15.6 µM) respectively.
authors.affiliation: Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Japan.
authors.forename: Lijun
authors.initials: L
authors.lastname: Xie
authors.forename: Xin
authors.initials: X
authors.lastname: Zhai
authors.forename: Lixiang
authors.initials: L
authors.lastname: Ren
authors.forename: Haiyan
authors.initials: H
authors.lastname: Meng
authors.forename: Chun
authors.initials: C
authors.lastname: Liu
authors.forename: Wufu
authors.initials: W
authors.lastname: Zhu
authors.forename: Yanfang
authors.initials: Y
authors.lastname: Zhao
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D019306:Artemisia / Q000737:chemistry*; D037621:Artemisinins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002599:Chalcone / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008958:Models, Molecular; D009369:Neoplasms / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D037621:Artemisinins; D002599:Chalcone; C031327:artemisinin