Novel spirobicyclic artemisinin analogues (artemalogues): Synthesis and antitumor activities
Liu, Gang2,3; Song, Shanshan1; Shu, Shiqi4; Miao, Zehong1; Zhang, Ao2,3; Ding, Chunyong2,3
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
2015-10-20
卷号103页码:17-28
关键词Artemisinin Spirobicyclic artemalogues 1,3-dipolar cycloaddition Stereoconfiguration Antiprolifereative effect
ISSN号0223-5234
DOI10.1016/j.ejmech.2015.08.035
文献子类Article
英文摘要The sesquiterpene lactone framework of artemisinin was used as a drug repositioning prototype for the development of novel antitumor drugs. Several series of novel artemisinin analogues (artemalogues) were designed and synthesized through 1,3-dipolar cycloaddition of artemisitene with nitrile oxides or nitrones. The isoxazolidine-containing spirobicyclic artemalogue 11b turns out to be the most potent with low micromolar IC50 values against all three tumor cells, which were at least 4- to 14-fold more potent than the parent artemisinin. (C) 2015 Elsevier Masson SAS. All rights reserved.
资助项目Pujiang Talent Project from Shanghai Commission of Science and Technology[14PJ1410700] ; Chinese NSF[81402790] ; Chinese NSF[81125021] ; Chinese NSF[81373277] ; Chinese NSF[81430080] ; National Program on Key Basic Research Project of China[2015CB910603-004]
WOS关键词LEUKEMIA-CELLS ; PLASMODIUM-FALCIPARUM ; ANTIMALARIAL ACTIVITY ; CANCER-CELLS ; DERIVATIVES ; CYTOTOXICITY ; HEME ; DIMERS ; AGENTS ; MOLECULES
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
WOS记录号WOS:000363344700002
内容类型期刊论文
源URL[http://119.78.100.183/handle/2S10ELR8/276356]  
专题药物化学研究室
中科院受体结构与功能重点实验室
新药研究国家重点实验室
通讯作者Ding, Chunyong
作者单位1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med SIMM, Shanghai 201203, Peoples R China;
2.Chinese Acad Sci, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China;
3.Chinese Acad Sci, Synthet Organ & Med Chem Lab, Shanghai Inst Mat Med SIMM, Shanghai 201203, Peoples R China;
4.China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China
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GB/T 7714
Liu, Gang,Song, Shanshan,Shu, Shiqi,et al. Novel spirobicyclic artemisinin analogues (artemalogues): Synthesis and antitumor activities[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2015,103:17-28.
APA Liu, Gang,Song, Shanshan,Shu, Shiqi,Miao, Zehong,Zhang, Ao,&Ding, Chunyong.(2015).Novel spirobicyclic artemisinin analogues (artemalogues): Synthesis and antitumor activities.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,103,17-28.
MLA Liu, Gang,et al."Novel spirobicyclic artemisinin analogues (artemalogues): Synthesis and antitumor activities".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 103(2015):17-28.
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