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
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出版日期 | 2004 |
卷号 | 87期号:7页码:1832-1853 |
ISSN号 | 0018-019X |
DOI | 10.1002/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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