4.6 Article

Effect of sunitinib derivatives on glioblastoma single-cell migration and 3D cell cultures

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AMERICAN JOURNAL OF CANCER RESEARCH
卷 13, 期 4, 页码 1377-1386

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E-CENTURY PUBLISHING CORP

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Sunitinib analogs; glioblastoma; tyrosine kinase inhibitors; spheroids; cell migration

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This study aimed to evaluate the anticancer activity of 16 new sunitinib derivatives in brain cancer cells (2D model) and spheroids (3D model). The compounds were assessed for their effects on cell viability, single-cell migration, and spheroid growth. EMAC4001 showed the highest reduction in viability for U-87MG and A-172 brain cancer cells. EMAC4001 exhibited the strongest inhibition of U-87MG cell migration, while EMAC4007 was most active in the A-172 cell line. Only sunitinib and EMAC4007 had a significant impact on spheroid growth in the respective cell lines.
This study aimed to evaluate the anticancer activity of 16 new sunitinib derivatives in brain cancer cells (2D model) and spheroids (3D model). The effect on cell viability was determined by the MTT assay. Single-cell migration assay was performed to examine the effect of selected compounds on individual cell migration. The activity of compounds in 3D cell cultures was examined by measuring the size change of spheroids formed using the Hanging drop method. The viability of brain cancer (U-87MG and A-172) cells was most reduced by compound EMAC4001. EMAC4001 showed the strongest effect on U-87MG cell migration, and EMAC4007 was the most active in the A-172 cell line. Only sunitinib had a statistically significant impact on spheroid growth at 100 nM and 500 nM concentrations in the U87-MG cell line and EMAC4007 had a statistically significant impact on A-172 spheroid growth at 100 nM and 500 nM concentrations, similarly to sunitinib.

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