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- W4211134489 abstract "Hypoxia-inducible factor (HIF)-1α is a key transcription factor that contributes to aggressive and drug-resistant phenotypes in tumor cells under hypoxic conditions. Therefore, targeting HIF-1α represents a promising therapeutic strategy for cancer drug development. In the present study, we designed, synthesized, and evaluated a new series of biarylquinoline derivatives as potential HIF-1α inhibitors based on structure-activity relationship. Among these derivatives, compound 7f represents the optimal agent with IC50 values of 28 nM and 15 nM in suppressing the viability of MiaPaCa-2 and MDA-MB-231 cells, respectively. Compound 7f also exhibited potent efficacy in inhibiting hypoxia-induced migration of MDA-MB-231 and MiaPaCa-2 cells. Mechanistically, compound 7f suppressed HIF-1α expression by blocking transcription and protein translation, in lieu of facilitating protein degradation. Moreover, this HIF-1α downregulation was associated with compound 7f's ability to concomitantly inhibit multiple signaling pathways governing HIF-1 α expression at different levels, including those mediated by STAT3, MEK/ERK MAPK, and mTOR/4E-BP1. Together, these findings underscore the translational potential of these biarylquinoline derivatives to be developed as novel HIF-1α inhibitors, which warrants further investigations." @default.
- W4211134489 created "2022-02-13" @default.
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- W4211134489 date "2022-04-01" @default.
- W4211134489 modified "2023-10-06" @default.
- W4211134489 title "Synthesis and evaluation of biarylquinoline derivatives as novel HIF-1α inhibitors" @default.
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- W4211134489 doi "https://doi.org/10.1016/j.bioorg.2022.105681" @default.
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