title: The application of tandem aza-wittig reaction to synthesize artemisinin-guanidine hybrids and their anti-tumor activity.
abstract: Three series of novel artemisinin-guanidine hybrids 4a-4f, 8a-8h and 9a-9h have been facilely synthesized via four-component reaction (aza-Wittig reaction) and evaluated for their anti-tumor activities against A549, HT-29 and MDA-MB-231 cell lines in vitro. All of the tested compounds showed enhanced anti-tumor activities with IC(50)  values ranging from 0.02 µM to 12.0 µM as compared to DHA (dihydroartemisinin). Among them, artemisinin derived dimers, compounds 9b (IC(50)  = 0.05 µM), 9d (IC(50)  = 0.06 µM) and 9f (IC(50)  = 0.02 µM) were found to be most active against HT29 cells.
authors: Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, P.R. China.
authors: Lijun
authors: L
authors: Xie
authors: Yanfang
authors: Y
authors: Zhao
authors: Xin
authors: X
authors: Zhai
authors: Peng
authors: P
authors: Li
authors: Chun
authors: C
authors: Liu
authors: Yangxiong
authors: Y
authors: Li
authors: Ping
authors: P
authors: Gong
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D037621:Artemisinins / Q000737:chemistry*; D001372:Aza Compounds / Q000737:chemistry*; D018929:Cell Culture Techniques; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D019791:Guanidine / Q000737:chemistry*; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D037621:Artemisinins; D001372:Aza Compounds; C031327:artemisinin; D019791:Guanidine