A. Kramell, Bianka Siewert, J. Wiese, V. Temml, H. Deigner, A. Al‐Harrasi, R. Csuk
{"title":"The cytotoxicity of brazilin and derivatives might be due to an inhibition of the c-Src-kinase","authors":"A. Kramell, Bianka Siewert, J. Wiese, V. Temml, H. Deigner, A. Al‐Harrasi, R. Csuk","doi":"10.13171/mjc10802010061536rc","DOIUrl":null,"url":null,"abstract":"In this study, several derivatives of brazilin with different lipophilicity were synthesized. The cytotoxic potential of these substances was evaluated in S.R.B. assays. A triacetylated brazilin reaction with PBr 3 or PCl 3 and a subsequent aqueous workup led to the formation of a phosphorous ester containing two triacetylated brazilin subunits. This compound held unexpected high cytotoxicity. In this study, Brazilin-derived triacetate showed good cytotoxic activity (EC50 = 5.2 M) concerning A2780 carcinoma cells. The results from docking studies suggest that brazilin's cytotoxicity might be due to an inhibition of a tyrosine kinase in an ATP-competitive manner.","PeriodicalId":18513,"journal":{"name":"Mediterranean Journal of Chemistry","volume":"89 1","pages":"790-798"},"PeriodicalIF":0.0000,"publicationDate":"2020-10-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"1","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Mediterranean Journal of Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.13171/mjc10802010061536rc","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 1
Abstract
In this study, several derivatives of brazilin with different lipophilicity were synthesized. The cytotoxic potential of these substances was evaluated in S.R.B. assays. A triacetylated brazilin reaction with PBr 3 or PCl 3 and a subsequent aqueous workup led to the formation of a phosphorous ester containing two triacetylated brazilin subunits. This compound held unexpected high cytotoxicity. In this study, Brazilin-derived triacetate showed good cytotoxic activity (EC50 = 5.2 M) concerning A2780 carcinoma cells. The results from docking studies suggest that brazilin's cytotoxicity might be due to an inhibition of a tyrosine kinase in an ATP-competitive manner.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
