Journal
ACS OMEGA
Volume 5, Issue 33, Pages 21181-21190Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.0c02916
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Funding
- National Natural Science Foundation of China [21572207, 21877101]
- Zhejiang Leading Innovation and Entrepreneurship Team [2018R01015]
- Zhejiang Provincial Natural Science Foundation of China [LY18B020020]
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In this study, we designed and synthesized a series of 3-(4-((5-((2-methylbipheny1-3-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 mu M, 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.
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