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- W3202324280 abstract "Blocking the programmed cell death protein 1 (PD-1) and programmed death-ligand (PD-L1) interaction has emerged as one of the most promising treatments for cancer immunotherapy. A novel series of compounds bearing a benzo[d]isoxazole scaffold was developed as PD-1/PD-L1 inhibitors, among them, compound P20 exhibited the most potent inhibitory activity, with an IC50 value of 26.8 nM. The preliminary structure-activity relationship was also investigated. The docking analysis of compound P20 with the PD-L1 dimer complex (PDB ID: 5j89) indicated that compound P20 was bound to the PD-L1 dimer with high affinity. These results suggest that compound P20 is a promising lead compound for the development of inhibitors of the PD-1/PD-L1 interaction." @default.
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- W3202324280 date "2021-11-01" @default.
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- W3202324280 title "Design, synthesis, and structure–activity relationship of PD-1/PD-L1 inhibitors with a benzo[d]isoxazole scaffold" @default.
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- W3202324280 doi "https://doi.org/10.1016/j.bmcl.2021.128403" @default.
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