光化学促进硼酸烷基酯与dna共轭芳基溴的交叉偶联反应用于dna编码文库合成。

IF 4 2区化学 Q1 BIOCHEMICAL RESEARCH METHODS

Bioconjugate Chemistry Pub Date : 2025-04-16 Epub Date: 2025-03-27 DOI:10.1021/acs.bioconjchem.4c00581

Baiyang Mu, Yiwei Zhang, Xudong Wang, Rui Jin, Weiwei Lu, Nidhal Selmi, Sixiu Liu, Avinash Bhat, Sara Pahlén, Giulia Bergonzini, Zhiqiang Duan, Yinan Song, Xiaojie Lu

{"title":"光化学促进硼酸烷基酯与dna共轭芳基溴的交叉偶联反应用于dna编码文库合成。","authors":"Baiyang Mu, Yiwei Zhang, Xudong Wang, Rui Jin, Weiwei Lu, Nidhal Selmi, Sixiu Liu, Avinash Bhat, Sara Pahlén, Giulia Bergonzini, Zhiqiang Duan, Yinan Song, Xiaojie Lu","doi":"10.1021/acs.bioconjchem.4c00581","DOIUrl":null,"url":null,"abstract":"The C(sp2)-C(sp3) cross-coupling reaction is an effective way to increase the C(sp3) content in compound collections for drug discovery, enhancing molecular diversity and offering a unique chemistry starting point. In this study, we report a mild, DNA-compatible, and off-DNA-inert photochemical cross-coupling reaction inspired by the amino radical transfer strategy. This method demonstrates broad substrate scopes for DNA-encoded library (DEL) constructions, utilizing commonly available structures on DNA and diverse alkyl boronate ester building blocks, which have not been widely applied in the current DEL chemical space.","PeriodicalId":29,"journal":{"name":"Bioconjugate Chemistry","volume":" ","pages":"718-723"},"PeriodicalIF":4.0000,"publicationDate":"2025-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Photochemical-Promoted Cross-Coupling Reaction of Alkyl Boronate Esters with DNA-Conjugated Aryl Bromides for DNA-Encoded Library Synthesis.\",\"authors\":\"Baiyang Mu, Yiwei Zhang, Xudong Wang, Rui Jin, Weiwei Lu, Nidhal Selmi, Sixiu Liu, Avinash Bhat, Sara Pahlén, Giulia Bergonzini, Zhiqiang Duan, Yinan Song, Xiaojie Lu\",\"doi\":\"10.1021/acs.bioconjchem.4c00581\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The C(sp2)-C(sp3) cross-coupling reaction is an effective way to increase the C(sp3) content in compound collections for drug discovery, enhancing molecular diversity and offering a unique chemistry starting point. In this study, we report a mild, DNA-compatible, and off-DNA-inert photochemical cross-coupling reaction inspired by the amino radical transfer strategy. This method demonstrates broad substrate scopes for DNA-encoded library (DEL) constructions, utilizing commonly available structures on DNA and diverse alkyl boronate ester building blocks, which have not been widely applied in the current DEL chemical space.\",\"PeriodicalId\":29,\"journal\":{\"name\":\"Bioconjugate Chemistry\",\"volume\":\" \",\"pages\":\"718-723\"},\"PeriodicalIF\":4.0000,\"publicationDate\":\"2025-04-16\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Bioconjugate Chemistry\",\"FirstCategoryId\":\"1\",\"ListUrlMain\":\"https://doi.org/10.1021/acs.bioconjchem.4c00581\",\"RegionNum\":2,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/3/27 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q1\",\"JCRName\":\"BIOCHEMICAL RESEARCH METHODS\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bioconjugate Chemistry","FirstCategoryId":"1","ListUrlMain":"https://doi.org/10.1021/acs.bioconjchem.4c00581","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/3/27 0:00:00","PubModel":"Epub","JCR":"Q1","JCRName":"BIOCHEMICAL RESEARCH METHODS","Score":null,"Total":0}

引用次数: 0

摘要

C(sp2)-C（sp3）交叉偶联反应是提高化合物中C（sp3）含量的有效途径，为药物发现提供了分子多样性和独特的化学起点。在这项研究中，我们报道了一种温和的、dna兼容的、非dna惰性的、由氨基自由基转移策略激发的光化学交叉偶联反应。该方法展示了DNA编码文库（DEL）构建的广泛底物范围，利用了DNA上常见的结构和各种烷基硼酸酯构建块，这些在当前的DEL化学领域尚未得到广泛应用。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

查看原文本刊更多论文

Photochemical-Promoted Cross-Coupling Reaction of Alkyl Boronate Esters with DNA-Conjugated Aryl Bromides for DNA-Encoded Library Synthesis.

The C(sp²)-C(sp³) cross-coupling reaction is an effective way to increase the C(sp³) content in compound collections for drug discovery, enhancing molecular diversity and offering a unique chemistry starting point. In this study, we report a mild, DNA-compatible, and off-DNA-inert photochemical cross-coupling reaction inspired by the amino radical transfer strategy. This method demonstrates broad substrate scopes for DNA-encoded library (DEL) constructions, utilizing commonly available structures on DNA and diverse alkyl boronate ester building blocks, which have not been widely applied in the current DEL chemical space.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Bioconjugate Chemistry 生物-化学综合

CiteScore

9.00

自引率

2.10%

发文量

236

审稿时长

1.4 months

期刊介绍： Bioconjugate Chemistry invites original contributions on all research at the interface between man-made and biological materials. The mission of the journal is to communicate to advances in fields including therapeutic delivery, imaging, bionanotechnology, and synthetic biology. Bioconjugate Chemistry is intended to provide a forum for presentation of research relevant to all aspects of bioconjugates, including the preparation, properties and applications of biomolecular conjugates.