Blocking of PD-1/PD-L1 with small molecules has been promising therapy for various cancers. In this work，based on hybrid approach we designed, synthesized and evaluated anticancer activity for thirty biphenyl-1,2,3-triazole hybrid analogues as follows. These results indicated that compounds 6d, 6e and 6h owned strong antiproliferative activity against three types of A549, MDA-MB-231 and HCC827 cancer cells, in particular against A549 cells. As well we evaluated their ability to block PD-1/PD-L1 interaction done by HTRF assay. Unfortunately, all the synthesized compounds presented slightly weak inhibition for PD-1/PD-L1 interaction.
biphenyl-1,2,3-triazole hybrid;PD-1/PD-L1 inhibitor;anti-tumor