| Autor: |
Suo, Yanrui, Xu, Min, Sun, Meimei, Lu, Weiwei, Wang, Xuan, Lu, Xiaojie |
| Zdroj: |
Organic Letters; December 2022, Vol. 24 Issue: 49 p9092-9096, 5p |
| Abstrakt: |
Indane and isoindoline are attractive bicyclic systems in biologically active compounds but are rarely reported in DNA-encoded libraries. In this paper, we reported an efficient and versatile approach for assembling indane and isoindoline scaffolds via a ruthenium-catalyzed [2 + 2 + 2] cyclotrimerization reaction. This method exhibits a broad substrate scope and has been successfully applied to construct a 53K-membered DNA-encoded library (DEL). In order to test its application, we carried out a preliminary selection of this DEL against Aurora A protein and identified a hit compound with 9.3 μM inhibition activity. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
|
