Eugenia Oleynik, Ekaterina Mikhina, D. Grigoreva, V. Maksimova, Lyubov Grebenkina, A. Matveev, E. Zhidkova, E. Lesovaya, Marianna Yakubovskaya
{"title":"Synephrine Analogues as Glucocorticoid Receptor Agonists","authors":"Eugenia Oleynik, Ekaterina Mikhina, D. Grigoreva, V. Maksimova, Lyubov Grebenkina, A. Matveev, E. Zhidkova, E. Lesovaya, Marianna Yakubovskaya","doi":"10.3390/ecsoc-27-16152","DOIUrl":null,"url":null,"abstract":": This work carried out the synthesis of several new synephrine analogues by universal method. Some of the synthesized compounds showed cytotoxicity on myeloid leukaemia cells K562 and lymphoma cell line Granta-519. Molecular docking using the glucocorticoid receptor (GR) model (PDB identifier 1P93) was performed to understand the possible underlying mechanism of compound action. The simulation showed the similarity of synephrine analogues’ binding to the binding of dexamethasone in the GR ligand-binding domain. The synthesized analogues exhibited cytotoxicity profiles similar to those of dexamethasone.","PeriodicalId":505262,"journal":{"name":"ECSOC 2023","volume":"411 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2023-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"ECSOC 2023","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3390/ecsoc-27-16152","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
: This work carried out the synthesis of several new synephrine analogues by universal method. Some of the synthesized compounds showed cytotoxicity on myeloid leukaemia cells K562 and lymphoma cell line Granta-519. Molecular docking using the glucocorticoid receptor (GR) model (PDB identifier 1P93) was performed to understand the possible underlying mechanism of compound action. The simulation showed the similarity of synephrine analogues’ binding to the binding of dexamethasone in the GR ligand-binding domain. The synthesized analogues exhibited cytotoxicity profiles similar to those of dexamethasone.