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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>

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New Kinase Inhibitors That Are Selectively Cytotoxic for Tumor Cells

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年4月12日

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  • D. A. Skvortsov,
  • I. V. Zhirkina,
  • D. A. Ipatova,
  • A. R. Pisarev,
  • A. S. Malyshev,
  • Y. A. Ivanenkov,
  • V. G. Kartsev,
  • O. A. Dontsova

摘要

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.