Gold(I)-Catalyzed Cascade Approach for the Synthesis of Tryptamine-Based Polycyclic Privileged Scaffolds as alpha(1)-Adrenergic Receptor Antagonists
文献类型：期刊论文
| 作者 | Li, Zeng1; Li, Jing2 ; Yang, Nan1; Chen, Ying2; Zhou, Yu1; Ji, Xun1; Zhang, Lei1; Wang, Jinfang1; Xie, Xin2; Liu, Hong1
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| 刊名 | JOURNAL OF ORGANIC CHEMISTRY
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| 出版日期 | 2013-11-01 |
| 卷号 | 78期号:21页码:10802-10811 |
| ISSN号 | 0022-3263 |
| DOI | 10.1021/jo4017887 |
| 文献子类 | Article |
| 英文摘要 | An efficient and facile gold(I)-catalyzed one-pot cascade protocol has been developed for the synthesis of tryptamine-fused polycyclic privileged structures through the treatment of substituted tryptamines and 2-ethynylbenzoic acids or 2-ethynylphenylacetic acids. This strategy features the formation of one C-C bond and two C-N bonds with high yields and broad substrate tolerance. The selected reduced target molecules are validated to perform as alpha(1)-adrenergic receptors antagonists. The most potent one, 4bh, exhibits an IC50 value of 277 nM on alpha(1A) subtype with a selectivity ratio of 15.8 over alpha(1B) subtype. |
| WOS关键词 | BENIGN PROSTATIC HYPERPLASIA ; SELECTIVE PDE5 INHIBITOR ; URINARY-TRACT SYMPTOMS ; ALZHEIMERS-DISEASE ; INDOLE ALKALOIDS ; DRUG DISCOVERY ; LIGANDS ; GOLD ; ANALOGS ; AFFINITIES |
| 资助项目 | National Natural Science Foundation of China[21021063] ; National Natural Science Foundation of China[91229204] ; National Natural Science Foundation of China[81025017] ; National S&T Major Projects[2012ZX09103101-072] ; National S&T Major Projects[2012ZX09301001-005] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000326615300022 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277402]  |
| 专题 | 国家新药筛选中心 药物化学研究室 |
| 通讯作者 | Xie, Xin |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Zeng,Li, Jing,Yang, Nan,et al. Gold(I)-Catalyzed Cascade Approach for the Synthesis of Tryptamine-Based Polycyclic Privileged Scaffolds as alpha(1)-Adrenergic Receptor Antagonists[J]. JOURNAL OF ORGANIC CHEMISTRY,2013,78(21):10802-10811. |
| APA | Li, Zeng.,Li, Jing.,Yang, Nan.,Chen, Ying.,Zhou, Yu.,...&Liu, Hong.(2013).Gold(I)-Catalyzed Cascade Approach for the Synthesis of Tryptamine-Based Polycyclic Privileged Scaffolds as alpha(1)-Adrenergic Receptor Antagonists.JOURNAL OF ORGANIC CHEMISTRY,78(21),10802-10811. |
| MLA | Li, Zeng,et al."Gold(I)-Catalyzed Cascade Approach for the Synthesis of Tryptamine-Based Polycyclic Privileged Scaffolds as alpha(1)-Adrenergic Receptor Antagonists".JOURNAL OF ORGANIC CHEMISTRY 78.21(2013):10802-10811. |
入库方式： OAI收割
来源：上海药物研究所
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