New Kinase Inhibitors That Are Selectively Cytotoxic for Tumor Cells

对肿瘤细胞具有选择性细胞毒性的新型激酶抑制剂

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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.

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