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- W4205127617 abstract "Abstract Purpose Signal transducer and activator of transcription 3 (STAT3) has been reported to be hyper-activated in triple-negative breast cancers (TNBCs) and predicts poor outcomes. However, no drugs targeting STAT3 have been marketed. To develop STAT3 inhibitors for the treatment of TNBC, we synthesized and evaluated a new series of naphthalene derivatives. Methods A new series of compounds with the scaffold of Selective Estrogen Receptor Modulator (SERM) and an amino group were designed and screened on the basis of the structure−activity relationship by MTT assay. The binding activity of SMY002 to STAT3 was predicted and validated by docking and SPR. The STAT3 signaling target and anti-cancer effect of SMY002 were evaluated by 3 three TNBC cell lines and the mice transplanted tumor model. Results Among the compounds, SMY002 (2a) displayed the most potent activity, which could directly interact with STAT3 SH2-domain, and strongly inhibit phosphorylation, dimerization, nuclear distribution, transcriptional activity, and target genes expression of STAT3. Furthermore, SMY002 markedly suppressed migration, invasion, survival, growth, and metastasis of TNBC cells in vitro and in vivo via down-regulating the expression of Cyclin D1 and MMP9. Conclusion The new compound SMY002 holds the potential of being developed into STAT3 inhibitory tools and TNBC treatment agents." @default.
- W4205127617 created "2022-01-26" @default.
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- W4205127617 date "2022-01-19" @default.
- W4205127617 modified "2023-09-28" @default.
- W4205127617 title "Synthesis and Evaluation of Naphthalene Derivatives as Potent STAT3 Inhibitors and Agents Against Triple-Negative Breast Cancer Growth and Metastasis" @default.
- W4205127617 doi "https://doi.org/10.21203/rs.3.rs-1238979/v1" @default.
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