{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Du F"],"funding":["National Natural Science Foundation of China","Liaoning Revitalization Talents Program"],"pagination":["E2059"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC7248849"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["25(9)"],"pubmed_abstract":["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 <b>L-04</b> improved both the H3K27Me3 reduction and antiproliferation parameters (IC<sub>50</sub> = 52.6 μM). These findings revealed that compound <b>L-04</b> is worthy of consideration as a lead compound to design more potent EZH2 inhibitors. During the preparation of compounds, we "],"journal":["Molecules (Basel, Switzerland)"],"pubmed_title":["5-Hydroxyindole-Based EZH2 Inhibitors Assembled via TCCA-Catalyzed Condensation and Nenitzescu Reactions."],"pmcid":["PMC7248849"],"funding_grant_id":["81973365","XLYC1902008","XLYC1908031"],"pubmed_authors":["Zhou Q","Du F","Wu C","Chen G","Sun W","Yang C","Wang L"],"additional_accession":[]},"is_claimable":false,"name":"5-Hydroxyindole-Based EZH2 Inhibitors Assembled via TCCA-Catalyzed Condensation and Nenitzescu Reactions.","description":"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 <b>L-04</b> improved both the H3K27Me3 reduction and antiproliferation parameters (IC<sub>50</sub> = 52.6 μM). These findings revealed that compound <b>L-04</b> is worthy of consideration as a lead compound to design more potent EZH2 inhibitors. During the preparation of compounds, we ","dates":{"release":"2020-01-01T00:00:00Z","publication":"2020 Apr","modification":"2026-05-02T05:14:14.869Z","creation":"2020-06-14T07:06:04Z"},"accession":"S-EPMC7248849","cross_references":{"pubmed":["32354194"],"doi":["10.3390/molecules25092059"]}}