473538-02-2Relevant academic research and scientific papers
Design, synthesis and biological evaluation of isoxazole-containing biphenyl derivatives as small-molecule inhibitors targeting the programmed cell death-1/ programmed cell death-ligand 1 immune checkpoint
Zhu, Peiyu,Zhang, Jian,Yang, Yifei,Wang, Lixun,Zhou, Jinpei,Zhang, Huibin
, p. 245 - 264 (2021/04/05)
Monoclonal antibodies targeting the programmed cell death-1/ programmed cell death-ligand 1 (PD-1/PD-L1) immune checkpoint have achieved enormous success in cancer immunotherapy. But the antibody-based immunotherapies carry a number of unavoidable deficie
Heterocyclic substituted biphenyl compound as well as preparation method and application thereof
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, (2021/08/28)
The invention discloses a heterocyclic substituted biphenyl compound as well as a preparation method and application thereof. According to the present invention, the compound can block the PD-1/PD-L1 signal pathway, and can be used as the immune checkpoint PD-1/PD-L1 small molecule inhibitor; and according to the compound disclosed by the invention, the metabolic stability is improved while the high binding rate with PD-L1 protein is maintained. A hydrophilic group is introduced to a heterocyclic ring, and the PD-1/PD-L1 inhibitory activity is improved.
