{"title":"Design, synthesis of schweinfurthin G derivatives and their biological evaluation as potential anticancer agents","authors":"","doi":"10.1016/j.tetlet.2024.155244","DOIUrl":null,"url":null,"abstract":"<div><p>Schweinfurthin G, one of the most potent of the schweinfurthins containing a hexahydroxanthene moiety, was found to exhibit strong cytotoxicity against A549 and KB cell lines with the IC<sub>50</sub> values of 0.8 μM and 0.6 μM, respectively. In this paper, a new series of schweinfurthin G derivatives modified on the isoprenyl side-chain were synthesized from schweinfurthin G using multicomponent reactions. The cytotoxicity of all the synthetic compounds was evaluated against four human cancer cell lines (KB, Hep3B, A549, MCF7) and one non-cancerous cell line (HEK293), which enabled to perform in-depth structure–activity relationships on a still poorly explored part of the molecule.</p></div>","PeriodicalId":438,"journal":{"name":"Tetrahedron Letters","volume":null,"pages":null},"PeriodicalIF":1.5000,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Tetrahedron Letters","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0040403924003393","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
引用次数: 0
Abstract
Schweinfurthin G, one of the most potent of the schweinfurthins containing a hexahydroxanthene moiety, was found to exhibit strong cytotoxicity against A549 and KB cell lines with the IC50 values of 0.8 μM and 0.6 μM, respectively. In this paper, a new series of schweinfurthin G derivatives modified on the isoprenyl side-chain were synthesized from schweinfurthin G using multicomponent reactions. The cytotoxicity of all the synthetic compounds was evaluated against four human cancer cell lines (KB, Hep3B, A549, MCF7) and one non-cancerous cell line (HEK293), which enabled to perform in-depth structure–activity relationships on a still poorly explored part of the molecule.
期刊介绍:
Tetrahedron Letters provides maximum dissemination of outstanding developments in organic chemistry. The journal is published weekly and covers developments in techniques, structures, methods and conclusions in experimental and theoretical organic chemistry. Rapid publication of timely and significant research results enables researchers from all over the world to transmit quickly their new contributions to large, international audiences.