Facile synthesis of pyridazinone-focused DNA-encoded libraries
文献类型：期刊论文
| 作者 | Lv, Yuhan4,5; Mu, Baiyang4,5; Qin, Shaozhao3; Wu, Xinyuan2,4; Lu, Weiwei4; Cui, Meiying1; Liu, Jiaxiang1; Wang, Xuan1; Lu, Xiaojie2,4
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| 刊名 | TETRAHEDRON LETTERS
 |
| 出版日期 | 2024-06-06 |
| 卷号 | 142页码:4 |
| ISSN号 | 0040-4039 |
| DOI | 10.1016/j.tetlet.2024.155076 |
| 通讯作者 | Liu, Jiaxiang() ; Wang, Xuan(wangxuan@alphama.com.cn) ; Lu, Xiaojie(xjlu@simm.ac.cn) |
| 英文摘要 | Employing pre-existing functionalized scaffolds to generate focused libraries exemplifies an expedited approach in terms of synthetic feasibility and efficiency. This strategic synthesis is particularly well-suited for scaffolds that are unattainable with DNA-compatible chemical tools. This manuscript utilizes pyridazinone as a paradigmatic scaffold to elucidate the synthetic workflow. Three functionalized pyridazinone reagents were obtained by conventional organic chemistries and then applied to prepare corresponding DNA-encoded libraries (DELs) by robust DNA-compatible reactions and abundant building blocks (BBs), ensuring both diversity and quality in the final libraries. The feasibility of these focused DELs were confirmed by subsequent affinity selection and off-DNA validation against the BRD4 target. |
| WOS关键词 | SCAFFOLD ; DESIGN |
| 资助项目 | Program for Interprofessional Practice, Education and Research, McMaster University[NSFC-91953203] ; Program for Interprofessional Practice, Education and Research, McMaster University[NSFC- 92253305] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001217834300001 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/311340]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Liu, Jiaxiang; Wang, Xuan; Lu, Xiaojie |
| 作者单位 | 1.Alphama Biotechnol Suzhou Co Ltd, 108 Yuxin Rd, Suzhou 215123, Jiangsu, Peoples R China 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, 138 Xianlin Rd, Nanjing 210023, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 501 Haike Rd,Zhang Jiang Hitech Pk, Shanghai 201203, Peoples R China 5.Shandong Second Med Univ, Weifang 261053, Shandong, Peoples R China |
| 推荐引用方式 GB/T 7714 | Lv, Yuhan,Mu, Baiyang,Qin, Shaozhao,et al. Facile synthesis of pyridazinone-focused DNA-encoded libraries[J]. TETRAHEDRON LETTERS,2024,142:4. |
| APA | Lv, Yuhan.,Mu, Baiyang.,Qin, Shaozhao.,Wu, Xinyuan.,Lu, Weiwei.,...&Lu, Xiaojie.(2024).Facile synthesis of pyridazinone-focused DNA-encoded libraries.TETRAHEDRON LETTERS,142,4. |
| MLA | Lv, Yuhan,et al."Facile synthesis of pyridazinone-focused DNA-encoded libraries".TETRAHEDRON LETTERS 142(2024):4. |
入库方式： OAI收割
来源：上海药物研究所
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