Discovery and Optimization of Novel Biphenyl Derivatives Bearing Cyclopropyl Linkage as Potent Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Inhibitors

A series of novel compounds bearing a cyclopropyl linkage were designed, synthesized, and evaluated as programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) inhibitors. An optimized compound (1S,2S)-A25 showed potent inhibitory activity against the PD-1/PD-L1 interaction (IC50 = 0.02...

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Veröffentlicht in:	Journal of medicinal chemistry 2023-05, Vol.66 (10), p.6811-6835
Hauptverfasser:	Jing, Tongfei, Zhang, Zhijing, Kang, Zhenghui, Mo, Jianshan, Yue, Xiaotong, Lin, Ziyou, Fu, Xiang, Liu, Chang, Ma, Hang, Zhang, Xiaolei, Hu, Wenhao
Format:	Artikel
Sprache:	eng
Schlagworte:	Apoptosis B7-H1 Antigen Humans Ligands Programmed Cell Death 1 Receptor - metabolism
Online-Zugang:	Volltext
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