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1 article(s) from Wang, Caiyi

Design, synthesis, and biological evaluation of FXR/ASK1 dual-target modulators

Xi Zhang,
Jingyan Wang,
Ziqiang Zhao,
Caiyi Wang,
Zenghui Ye,
Wei-Yuan Ma,
Jian-Xing Xu and
Fengzhi Zhang

Beilstein J. Org. Chem. 2026, 22, 771–781, doi:10.3762/bjoc.22.59

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Scheme 1: Steroidal and nonsteroidal FXR agonists.

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Scheme 2: ASK1 inhibitors.

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Scheme 3: Dual FXR/ASK1 modulation strategy for MASH.

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Scheme 4: Synthesis of compound 2. Conditions: (a) NH₂OH·HCl, NaOH, EtOH/H₂O, 70 °C, 12 h; (b) NCS, DMF, 40 °...

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Scheme 5: Synthesis of compounds IXa–d. Conditions: (a) N₂H₄·H₂O, MeOH, rt, 12 h; (b) DMF–DMA, 80 °C, 12 h; (...

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Scheme 6: Synthesis of compounds Z1–15. Conditions: (a) K₂CO₃, KI, MeCN, 50 °C, 6 h, 86–96% yield; (b) Pd₂(db...

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Scheme 7: Synthesis of compounds Z16–29. Conditions: (a) Pd(PPh₃)₄, Na₂CO₃, 1,4-dioxane/H₂O, 80 °C, 18 h, 64–...

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Scheme 8: Synthesis of compound Z30. Conditions: (a) NaH, DMF, rt, 16 h; (b) TFA, DCM, 0 °C, 3 h; (c) Pd₂(dba)...

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Scheme 9: Molecular docking of dual-target modulator Z8 to the ligand binding sites of FXR (PDB ID: 3DCT, htt...

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Figure 1: FXR agonist activity of all compounds. Results of the dual-luciferase reporter assay in CHO cells c...

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Figure 2: ASK1 inhibition of all compounds. Results of the ADP-Glo™ kinase assay after treating ASK1 kinase w...

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Figure 3: Effects of Z8 and Z30 on OA-induced lipid accumulation in HepG2 cells. Cells were treated with GW40...

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Published 20 May 2026

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