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• W3049580678 abstract "In this study, we designed and synthesized a series of 3-(4-((5-((2-methylbiphenyl-3-yl) methoxy)-2-(piperazin-1-ylmethyl)phenoxy)methyl)-1H-1,2,3-triazol-1-yl)benzonitrile derivatives and examined the effect of the compounds on the interaction between PD-1 and PD-L1. Among the newly synthesized compounds, compound 7 exhibited the most potent inhibitory activity for PD-1/PD-L1 binding, with an IC50 value being 8.52 μM, through homogeneous time-resolved fluorescence (HTRF) assay. Docking studies indicated that compound 7 can very well interact with PD-L1 dimerization like BMS-202 as a positive control, consistent with the results of the HTRF assay. Compound 7 is thus a promising candidate for further optimization as an inhibitor of the PD-1/PD-L1 signaling pathway." @default.
• W3049580678 created "2020-08-21" @default.
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• W3049580678 date "2020-08-14" @default.
• W3049580678 modified "2023-10-18" @default.
• W3049580678 title "Synthesis and Evaluation of Biphenyl-1,2,3-Triazol-Benzonitrile Derivatives as PD-1/PD-L1 Inhibitors" @default.
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• W3049580678 doi "https://doi.org/10.1021/acsomega.0c02916" @default.
• W3049580678 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7450630" @default.
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