Streamlined construction of peptide macrocycles via palladium-catalyzed intramolecular S-arylation in solution and on DNA
文献类型：期刊论文
| 作者 | Yang, Peng1,2; Wang, Xuan3; Li, Bo1,2; Yang, Yixuan3; Yue, Jinfeng3; Suo, Yanrui3; Tong, Huarong1,2; He, Gang1,2; Lu, Xiaojie3 ; Chen, Gong1,2
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| 刊名 | CHEMICAL SCIENCE
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| 出版日期 | 2021-04-28 |
| 卷号 | 12期号:16页码:5804-5810 |
| ISSN号 | 2041-6520 |
| DOI | 10.1039/d1sc00789k |
| 文献子类 | Article |
| 英文摘要 | A highly efficient and versatile method for construction of peptide macrocycles via palladium-catalyzed intramolecular S-arylation of alkyl and aryl thiols with aryl iodides under mild conditions is developed. The method exhibits a broad substrate scope for thiols, aryl iodides and amino acid units. Peptide macrocycles of a wide range of size and composition can be readily assembled in high yield from various easily accessible building blocks. This method has been successfully employed to prepare an 8-million-membered tetrameric cyclic peptide DNA-encoded library (DEL). Preliminary screening of the DEL library against protein p300 identified compounds with single digit micromolar inhibition activity. |
| WOS关键词 | LIBRARY |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000631581200001 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309394]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | He, Gang; Lu, Xiaojie; Chen, Gong |
| 作者单位 | 1.Nankai Univ, Coll Chem, State Key Lab, Tianjin 300071, Peoples R China; 2.Nankai Univ, Coll Chem, Inst Elementoorgan Chem, Tianjin 300071, Peoples R China; 3.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, 501 Haike Rd,Zhang Jiang Hitech Pk, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Peng,Wang, Xuan,Li, Bo,et al. Streamlined construction of peptide macrocycles via palladium-catalyzed intramolecular S-arylation in solution and on DNA[J]. CHEMICAL SCIENCE,2021,12(16):5804-5810. |
| APA | Yang, Peng.,Wang, Xuan.,Li, Bo.,Yang, Yixuan.,Yue, Jinfeng.,...&Chen, Gong.(2021).Streamlined construction of peptide macrocycles via palladium-catalyzed intramolecular S-arylation in solution and on DNA.CHEMICAL SCIENCE,12(16),5804-5810. |
| MLA | Yang, Peng,et al."Streamlined construction of peptide macrocycles via palladium-catalyzed intramolecular S-arylation in solution and on DNA".CHEMICAL SCIENCE 12.16(2021):5804-5810. |
入库方式： OAI收割
来源：上海药物研究所
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