101782-20-1Relevant articles and documents
5-Hydroxyindole-based EZH2 inhibitors assembled via TCCA-catalyzed condensation and Nenitzescu reactions
Chen, Guoliang,Du, Fangyu,Sun, Wenjiao,Wang, Lihui,Wu, Chunfu,Yang, Cheng,Zhou, Qifan
, (2020/05/16)
5-Hydroxyindole derivatives have various demonstrated biological activities. Herein, we used 5-hydroxyindole as a synthetic starting point for structural alterations in a combinatorial process to synthesize 22 different compounds with EZH2 inhibitor pharmacophores. A series of 5-hydroxyindole-derived compounds were screened inhibitory activities against K562 cells. According to molecular modeling and in vitro biological activity assays, the preliminary structure-activity relationship was summarized. Compound L–04 improved both the H3K27Me3 reduction and antiproliferation parameters (IC50 = 52.6 μM). These findings revealed that compound L–04 is worthy of consideration as a lead compound to design more potent EZH2 inhibitors. During the preparation of compounds, we discovered that trichloroisocyanuric acid (TCCA) is a novel catalyst which demonstrates condensation-promoting effects. To gain insight into the reaction, in situ React IR technology was used to confirm the reactivity. Different amines were condensed in high yields with β-diketones or β-ketoesters in the presence of TCCA to afford the corresponding products in a short time (10~20 min), which displayed some advantages and provided an alternative condensation strategy.
5-HYDROXY-4-AMINOMETHYL-1-CYCLOHEXANE OR (CYCLOHEPTYL)--3-ALKOXYCARBONYL INDOLE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE ANTIVIRAL SALTS THEREOF AND A METHOD FOR THE PRODUCTION THEREOF
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Page/Page column 7, (2011/02/19)
The invention relates to novel 5-hydroxy-4-aminomethyl-1-cyclohexane or (cycloheptyl)--3-alkoxycarbonyl indole derivatives of general formula (I) and to pharmaceutically acceptable salts thereof exhibiting antiviral activity and to a method for the produc
