Design, Synthesis, and Antitumor Activity Evaluation of 2-Arylmethoxy-4-(2,2′-dihalogen-substituted biphenyl-3-ylmethoxy) Benzylamine Derivatives as Potent PD-1/PD-L1 Inhibitors

Abstract excerpt

Novel 2-arylmethoxy-4-(2,2′-dihalogen-substituted biphenyl-3-ylmethoxy) benzylamine derivatives were designed, synthesized, and evaluated in vitro and in vivo against cancers as PD-1/PD-L1 inhibitors. Through the computer-aided structural optimization and the homogeneous time-resolved fluorescence (HTRF) assay, compound A56 was found to most strongly block the PD-1/PD-L1 interaction with an IC 50 value of 2.4 ±...

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