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学科主题: 药学
题名:
Synthesis and Antitumor Activity Evaluation of gamma-Monofluorinated and gamma,gamma-Difluorinated Goniothalamin Analogues
作者: Yang, Yi1; Yang, Zhenjun3; Cheng, Chunru1; Qing, Fengling2
关键词: Goniothalamin ; Stille coupling ; fluorine ; antitumor activity
刊名: CHINESE JOURNAL OF CHEMISTRY
发表日期: 2013-06-01
DOI: 10.1002/cjoc.201300227
卷: 31, 期:6, 页:805-812
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Multidisciplinary
研究领域[WOS]: Chemistry
关键词[WOS]: GEM-DIFLUOROMETHYLENATED ANALOGS ; RING-CLOSING METATHESIS ; BRYONOPSIS-LACINIOSA ; MEDICINAL CHEMISTRY ; CYTOTOXIC ACTIVITY ; COUPLING REACTIONS ; STYRYL-LACTONES ; DRUG DESIGN ; FLUORINE ; ORGANOSTANNANES
英文摘要:

A series of novel ,-difluorinated Goniothalamin analogues 4a-4i and 6a-6i were synthesized. The key steps included the construction of C-5 stereocenter adjacent to gem-difluoromethylene group by way of lipase AK catalyzed kinetic resolution, the introduction of aryl group via Stille coupling, and lactonization by 1,5-oxidative cyclization. These ,-difluorinated Goniothalamin analogues 4a-4i and their enantiomers 6a-6i, together with several corresponding -monofluorinated Goniothalamin analogues were biologically evaluated against four different cancer cell lines. Compound 7h showed a nearly equivalent potency as the parent (R)-Goniothalamin in the micromolar range. The different fluorine effects between fluoromethylene and gem-difluoromethylene on antitumor activity were discussed through the analysis of bioassay data.

语种: 英语
所属项目编号: 2107028 ; 20832008 ; 2012CB821600 ; 2012RC17 ; 2012RC15
项目资助者: National Natural Science Foundation of China ; National Basic Research Program of China ; Scientific Research Program of Sichuan University of Science Engineering
WOS记录号: WOS:000320392400017
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59724
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Sichuan Univ Sci & Engn, Sch Chem & Pharmaceut Engn, Zigong 643000, Sichuan, Peoples R China
2.Chinese Acad Sci, Key Lab Organofluorine Chem, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China
3.Peking Univ, State Key Lab Nat & Biomimet Drugs, Sch Pharmaceut Sci, Beijing 100083, Peoples R China

Recommended Citation:
Yang, Yi,Yang, Zhenjun,Cheng, Chunru,et al. Synthesis and Antitumor Activity Evaluation of gamma-Monofluorinated and gamma,gamma-Difluorinated Goniothalamin Analogues[J]. CHINESE JOURNAL OF CHEMISTRY,2013,31(6):805-812.
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