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• W4310191808 endingPage "110286" @default.
• W4310191808 startingPage "110286" @default.
• W4310191808 abstract "In order to discover more effective and less toxic drugs in the field of anti-tumor, the backbone structure of 17β-estradiol was modified, and 11 target compounds were synthesized. Compounds 5 and 10, which exhibited better anti-tumor activity and higher selectivity (more than 10-fold), were chosen for further biological investigation. Flow cytometry results indicated that 5 and 10 could arrest MCF-7 cells in the G2 phase and induce apoptosis. Immunohistochemical analysis revealed that 5 and 10 could bind to the estradiol receptor alpha in MCF-7 cells. Western blotting and real-time PCR assays were performed to detect the effects of compounds on apoptosis-related targets at the protein and gene levels. These results showed that both 5 and 10 could dosed-dependently increase the expression of Apaf-1, Bax, caspase-3,8,9 and reduce the expression levels of the anti-apoptotic factors Bcl-2 and Bcl-xL. Besides, the Human apoptosis array assay demonstrated the expression level of death receptor Trail R2/DR5 was upregulated obviously while the expression of TNF R1, IAPs and Hsp27/60/70 were downregulated. On the whole, 5 induced MCF-7 cell death through the endogenous pathway in mitochondria and the exogenous pathway with death receptor Trail R2/DR5." @default.
• W4310191808 created "2022-11-30" @default.
• W4310191808 creator A5013606129 @default.
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• W4310191808 date "2023-01-01" @default.
• W4310191808 modified "2023-10-04" @default.
• W4310191808 title "(4-Picolylamino)-17β-Estradiol derivative and analogues induce apoptosis with death receptor trail R2/DR5 in MCF-7" @default.
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• W4310191808 doi "https://doi.org/10.1016/j.cbi.2022.110286" @default.
• W4310191808 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36460128" @default.
• W4310191808 hasPublicationYear "2023" @default.
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