基于 DNA 的炔烃碘化和炔基偶联作为 DEL 合成的有用工具。
On-DNA Alkyne Iodination and Acetylenic Coupling as a Useful Tool for DEL Synthesis.
机构信息
Pharmaron (Ningbo) Technology Development Co., Ltd. No. 800 Bin-Hai 4th Road, Hangzhou Bay New Zone, Ningbo, 315336, China.
Pharmaron Beijing Co., Ltd., 6 Taihe Road, BDA, Beijing, 100176, China.
出版信息
Bioconjug Chem. 2022 Dec 21;33(12):2299-2306. doi: 10.1021/acs.bioconjchem.2c00471. Epub 2022 Nov 30.
1-Iodoalkynes and 1,3-diynes are versatile chemical intermediates and pharmaceutically valuable ingredients. In this study, copper mediated on-DNA alkyne iodination and Cadiot-Chodkiewicz coupling are developed for the first time. This generates diverse, systematic, and unprecedented topographic structural features, which could be invaluable as molecular recognition agents for drug discovery in DEL screening.
1-碘炔和 1,3-二炔是多功能的化学中间体和具有药用价值的成分。在这项研究中，首次开发了铜介导的 DNA 上炔基碘化和 Cadiot-Chodkiewicz 偶联。这产生了多样化、系统和前所未有的地形结构特征，这些特征可能作为 DEL 筛选中药物发现的分子识别剂非常有价值。
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