D. A. Skvortsov, I. V. Zhirkina, D. A. Ipatova, A. R. Pisarev, A. S. Malyshev, Y. A. Ivanenkov, V. G. Kartsev, O. A. Dontsova
{"title":"New Kinase Inhibitors That Are Selectively Cytotoxic for Tumor Cells","authors":"D. A. Skvortsov, I. V. Zhirkina, D. A. Ipatova, A. R. Pisarev, A. S. Malyshev, Y. A. Ivanenkov, V. G. Kartsev, O. A. Dontsova","doi":"10.1134/S1607672924601446","DOIUrl":null,"url":null,"abstract":"<p>To search for substances selectively acting on tumor cells, phenotypic screening in a coculture of tumor cells with non-tumor cells was used in the work. The compound STOCK7S-36520, selectively cytotoxic in the coculture of breast tumor cells MCF7' and non-tumor MCF10A cells, contains structural elements characteristic of kinase inhibitors. Analysis of the compound STOCK7S-36520 and its derivative STOCK7S-47016 showed that they are new multikinase inhibitors. The highest inhibition of 84% was shown by compound STOCK7S-47016 against GCK kinase. Of interest is the significant selectivity of action against some of the cell lines studied: the selectivity index of STOCK7S-36520 against the prostate tumor cell line PC3 is 29 times compared to the model line of non-tumor fibroblasts VA13.</p>","PeriodicalId":529,"journal":{"name":"Doklady Biochemistry and Biophysics","volume":"521 1","pages":"239 - 245"},"PeriodicalIF":0.8000,"publicationDate":"2025-04-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1134/S1607672924601446.pdf","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Doklady Biochemistry and Biophysics","FirstCategoryId":"99","ListUrlMain":"https://link.springer.com/article/10.1134/S1607672924601446","RegionNum":4,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
To search for substances selectively acting on tumor cells, phenotypic screening in a coculture of tumor cells with non-tumor cells was used in the work. The compound STOCK7S-36520, selectively cytotoxic in the coculture of breast tumor cells MCF7' and non-tumor MCF10A cells, contains structural elements characteristic of kinase inhibitors. Analysis of the compound STOCK7S-36520 and its derivative STOCK7S-47016 showed that they are new multikinase inhibitors. The highest inhibition of 84% was shown by compound STOCK7S-47016 against GCK kinase. Of interest is the significant selectivity of action against some of the cell lines studied: the selectivity index of STOCK7S-36520 against the prostate tumor cell line PC3 is 29 times compared to the model line of non-tumor fibroblasts VA13.
期刊介绍：
Doklady Biochemistry and Biophysics is a journal consisting of English translations of articles published in Russian in biochemistry and biophysics sections of the Russian-language journal Doklady Akademii Nauk. The journal''s goal is to publish the most significant new research in biochemistry and biophysics carried out in Russia today or in collaboration with Russian authors. The journal accepts only articles in the Russian language that are submitted or recommended by acting Russian or foreign members of the Russian Academy of Sciences. The journal does not accept direct submissions in English.
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