中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Synthesis of A/B ring analogs of territrem B and evaluation of their biological activities

文献类型:期刊论文

作者Zhao, JH; Zhao, F; Wang, YG; Li, HB; Zhang, QJ; Guenard, D; Ge, QF; Weir, EQ; Jiang, H; Wu, YH
刊名HELVETICA CHIMICA ACTA
出版日期2004
卷号87期号:7页码:1832-1853
ISSN号0018-019X
DOI10.1002/hlca.200490163
文献子类Article
英文摘要Two series of territrem B analogs, i.e., 5 - 10, containing both the 2-en-1-one-A-ring and the aromatic-E-ring pharmacophores were designed and synthesized from jujubogenin (4a). The anti-acetylcholinesterase (anti-AChE), anti-caspase-3, and other biological activities of these territrem-B analogs and their intermediates were assessed. Compound 9b, 22a, and 24f were shown to be weak inhibitors of AChE. None of the synthesized compounds exhibited significant inhibitory activity on caspase-3. On the other hand, compounds 22e, 24a, 7b, and 8a showed mild cytotoxicity on cultured KB cells, with IC50, values of 2.0, 3.5, 6.5, and 14 mum, respectively. In addition, compounds 23b and 5f were active against injury arising from oxygen-glucose deprivation.
WOS关键词SELECTIVE ACETYLCHOLINESTERASE INHIBITORS ; PENICILLIUM SP FO-4259 ; OXYGEN-GLUCOSE DEPRIVATION ; RAT CORTICAL-NEURONS ; ALZHEIMERS-DISEASE ; ANTIACETYLCHOLINESTERASE ACTIVITY ; CHOLINERGIC HYPOTHESIS ; DIRECT OXIDATION ; ARISUGACIN-A ; HUPERZINE-A
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000223221900017
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/274135]  
专题中国科学院上海药物研究所
通讯作者Zhao, JH
作者单位1.CNRS, Inst Chim Subst Nat, F-91198 Gif Sur Yvette, France
2.Zhejiang Univ, Coll Med, Hangzhou 310031, Peoples R China
3.Dali Coll, Sch Pharm, Dali 671000, Peoples R China
4.Zhejiang Hisun Nat Pharmaceut R&D Co Ltd, Hangzhou 310006, Peoples R China
5.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 200031, Peoples R China
6.Natl Taiwan Univ, Coll Med, Sch Pharm, Taipei 10018, Taiwan
7.Chinese Univ Hong Kong, Dept Biochem, Shatin, Hong Kong, Peoples R China
8.Zhejiang Univ, Coll Pharmaceut Sci, Dept Trad Chinese Med & Nat Drug Res, Hangzhou 310031, Peoples R China
9.Zhejiang Univ, Dept Chem, Hangzhou 310027, Peoples R China
推荐引用方式
GB/T 7714
Zhao, JH,Zhao, F,Wang, YG,et al. Synthesis of A/B ring analogs of territrem B and evaluation of their biological activities[J]. HELVETICA CHIMICA ACTA,2004,87(7):1832-1853.
APA Zhao, JH.,Zhao, F.,Wang, YG.,Li, HB.,Zhang, QJ.,...&Zhao, Y.(2004).Synthesis of A/B ring analogs of territrem B and evaluation of their biological activities.HELVETICA CHIMICA ACTA,87(7),1832-1853.
MLA Zhao, JH,et al."Synthesis of A/B ring analogs of territrem B and evaluation of their biological activities".HELVETICA CHIMICA ACTA 87.7(2004):1832-1853.

入库方式: OAI收割

来源:上海药物研究所

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