Clickable Selenylation – a Paradigm for Seleno‐Medicinal Chemistry
Clickable Selenylation – a Paradigm for Seleno‐Medicinal Chemistry
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可点击的硒化作用 — Seleno 的范例 — 药物化学
DOI：
10.1002/cmdc.202200324
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发表时间：
2022-07
期刊：
影响因子：
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通讯作者：
Hongtao Xu
中科院分区：
文献类型：
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作者：
Wei Hou;Hewei Dong;Ying Yao;Kangyin Pan;Guang Yang;Peixiang Ma;Hongtao Xu
硒（Se）是药物化学中一种新兴的多功能参与者。将硒掺入小分子和天然产物中可能具有多种益处。然而，含硒化合物库的合成缺乏有效的方法，极大地阻碍了硒药物化学的发展。为了解决这一问题，我们提出了开发可点击的硒化反应，可用于含硒原位文库和DNA编码文库（SeDEL）的合成，从而快速产生超大规模的含硒化合物库，促进硒药物化学的发展。该研究范式可以归纳为可点击的硒化化学开发→原位文库构建/SeDEL合成→基于表型或靶点的筛选→硒命中化合物。
Selenium (Se) is an emerging versatile player in medicinal chemistry. The incorporation of Se into small molecules and natural products could have multiple benefits. However, the lack of efficient methods for the synthesis of Se-containing chemical library has greatly hindered the development of seleno-medicinal chemistry. With the aim to address this issue, we proposed the development of clickable selenylation reactions, which can be used in the synthesis of Se-containing in situ library and DNA-encoded library (SeDEL), thereby quickly producing ultra-large collections of Se-containing compounds and boosting the development of seleno-medicinal chemistry. This research paradigm can be concluded as clickable selenylation chemistry development→in situ library construction/SeDEL synthesis→phenotype- or target-based screening→seleno-hit compound.