Synthesis and biological evaluation of immunosuppressive agent DZ2002 and its stereoisomers
文献类型：期刊论文
| 作者 | Zhang, Yang-Ming1,2,3 ; Ding, Yu4; Tang, Wei4; Luo, Wei3; Gu, Min3; Lu, Wei1,2; Tang, Jie1,2; Zuo, Jian-Ping4; Nan, Fa-Jun3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
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| 出版日期 | 2008-10-15 |
| 卷号 | 16期号:20页码:9212-9216 |
| 关键词 | DZ2002 stereoisomers synthesis immunosuppressive potency S-adenosyl-L-homocysteine hydrolase |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2008.09.017 |
| 文献子类 | Article |
| 英文摘要 | DZ2002 and its related stereoisomers were efficiently synthesized. The optical data of (R)- and (S)-DZ2002 were disclosed here for the first time. Their inhibitory potency was evaluated on SAHase and MLR assay in the mean time. In accordance with respective inhibitory potency of SAHase, the immunosuppressive potency order was demonstrated as (S)-Z2002 > (Rac)-DZ2002 > (R)-DZ2002 > (Keto)DZ2002. These results indicate (S)-configuration of 2-chiral center in DZ2002 is important for binding with SAHase. (C) 2008 Elsevier Ltd. All rights reserved. |
| WOS关键词 | L-HOMOCYSTEINE HYDROLASE ; T-CELL-ACTIVATION ; S-ADENOSYLMETHIONINE ; INHIBITION |
| 资助项目 | National Natural Science Foundation of China[30725049] ; Shanghai Commission of Science and Technology[064319014] ; New Century Excellent Talents in University[00000000] ; [30572195] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000259973200016 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272780]  |
| 专题 | 药理学第一研究室 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 国家新药筛选中心 |
| 通讯作者 | Lu, Wei |
| 作者单位 | 1.E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China; 2.E China Normal Univ, Inst Med Chem, Shanghai 200062, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Dept Immunopharmacol, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Yang-Ming,Ding, Yu,Tang, Wei,et al. Synthesis and biological evaluation of immunosuppressive agent DZ2002 and its stereoisomers[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2008,16(20):9212-9216. |
| APA | Zhang, Yang-Ming.,Ding, Yu.,Tang, Wei.,Luo, Wei.,Gu, Min.,...&Nan, Fa-Jun.(2008).Synthesis and biological evaluation of immunosuppressive agent DZ2002 and its stereoisomers.BIOORGANIC & MEDICINAL CHEMISTRY,16(20),9212-9216. |
| MLA | Zhang, Yang-Ming,et al."Synthesis and biological evaluation of immunosuppressive agent DZ2002 and its stereoisomers".BIOORGANIC & MEDICINAL CHEMISTRY 16.20(2008):9212-9216. |
入库方式： OAI收割
来源：上海药物研究所
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