A. Kramell, Bianka Siewert, J. Wiese, V. Temml, H. Deigner, A. Al‐Harrasi, R. Csuk
{"title":"巴西林及其衍生物的细胞毒性可能是由于对c- src激酶的抑制作用","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":"{\"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}","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}
The cytotoxicity of brazilin and derivatives might be due to an inhibition of the c-Src-kinase
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.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
