Diversified strategy for the synthesis of DNA-encoded oxindole libraries
Wang, Xuan1,2; Liu, Jiaxiang1; Yan, Ziqin1; Liu, Xiaohong3,4,5; Liu, Sixiu1; Suo, Yanrui1; Lu, Weiwei1; Yue, Jinfeng1; Chen, Kaixian3,4,5; Jiang, Hualiang3,4,5
2021-02-28
发表期刊CHEMICAL SCIENCE
ISSN2041-6520
EISSN2041-6539
卷号12期号:8页码:2841-2847
DOI10.1039/d0sc06696f
摘要DNA-encoded library technology (DELT) employs DNA as a barcode to track the sequence of chemical reactions and enables the design and synthesis of libraries with billions of small molecules through combinatorial expansion. This powerful technology platform has been successfully demonstrated for hit identification and target validation for many types of diseases. As a highly integrated technology platform, DEL is capable of accelerating the translation of synthetic chemistry by using on-DNA compatible reactions or off-DNA scaffold synthesis. Herein, we report the development of a series of novel on-DNA transformations based on oxindole scaffolds for the design and synthesis of diversity-oriented DNA-encoded libraries for screening. Specifically, we have developed 1,3-dipolar cyclizations, cyclopropanations, ring-opening of reactions of aziridines and Claisen-Schmidt condensations to construct diverse oxindole derivatives. The majority of these transformations enable a diversity-oriented synthesis of DNA-encoded oxindole libraries which have been used in the successful hit identification for three protein targets. We have demonstrated that a diversified strategy for DEL synthesis could accelerate the application of synthetic chemistry for drug discovery.
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收录类别SCIE ; EI ; IC
语种英语
WOS研究方向Chemistry
WOS类目Chemistry, Multidisciplinary
WOS记录号WOS:000625958900008
出版者ROYAL SOC CHEMISTRY
原始文献类型Article
引用统计
文献类型期刊论文
条目标识符https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/126175
专题生命科学与技术学院_博士生
生命科学与技术学院_特聘教授组_陈凯先组
免疫化学研究所_特聘教授组_蒋华良组
通讯作者Zhao, Yujun; Zheng, Mingyue; Dai, Dongcheng; Lu, Xiaojie
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 501 Haike Rd,Zhang Jiang Hitech Pk, Shanghai 201203, Peoples R China;
2.Amgen Biopharmaceut R&D Shanghai Co Ltd, Amgen Asia R&D Ctr, 4560 Jinke Rd,Bldg 2,13th Floor, Shanghai 201210, Peoples R China;
3.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai Inst Adv Immunochem Studies, Shanghai 201210, Peoples R China;
4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discovery & Design Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China;
5.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
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Wang, Xuan,Liu, Jiaxiang,Yan, Ziqin,et al. Diversified strategy for the synthesis of DNA-encoded oxindole libraries[J]. CHEMICAL SCIENCE,2021,12(8):2841-2847.
APA Wang, Xuan.,Liu, Jiaxiang.,Yan, Ziqin.,Liu, Xiaohong.,Liu, Sixiu.,...&Lu, Xiaojie.(2021).Diversified strategy for the synthesis of DNA-encoded oxindole libraries.CHEMICAL SCIENCE,12(8),2841-2847.
MLA Wang, Xuan,et al."Diversified strategy for the synthesis of DNA-encoded oxindole libraries".CHEMICAL SCIENCE 12.8(2021):2841-2847.
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