Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 52287-51-1, is researched, Molecular C8H7BrO2, about Novel Biphenyl Pyridines as Potent Small-Molecule Inhibitors Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction, the main research direction is biphenyl pyridine preparation PD1 PDL1 inhibition antitumor SAR pharmacokinetics.HPLC of Formula: 52287-51-1.
The design, synthesis and in-vitro and in-vivo evaluation of a series of novel biphenyl pyridines, I [R = Ph, 3-methoxyphenyl, 1,3-benzodioxol-5-yl, etc.; R1 = H, (2-hydroxyethylamino)methyl; R2 = methoxycarbonyl, (2-hydroxyethylamino)methyl, [[(2S)-5-oxopyrrolidin-2-yl]methylamino]methyl, etc.; R3 = H, MeO] as the inhibitors of PD-1/PD-L1 was reported. Compound I [R = Ph, R1 = H, R2 = (2-hydroxyethylamino)methyl, R3 = MeO] was found to inhibit the PD-1/PD-L1 interaction with an IC50 value of 3.8 ± 0.3 nM and enhance the killing activity of tumor cells by immune cells. Compound I [R = Ph, R1 = H, R2 = (2-hydroxyethylamino)methyl, R3 = MeO] displayed great pharmacokinetics (oral bioavailability of 22%) and significant in-vivo antitumor activity in a CT26 mouse model. Flow cytometry and immunohistochem. data indicated that compound I [R = Ph, R1 = H, R2 = (2-hydroxyethylamino)methyl, R3 = MeO] activates the immune activity in tumors. These results suggest that compound I [R = Ph, R1 = H, R2 = (2-hydroxyethylamino)methyl, R3 = MeO] is a promising small-mol. inhibitor against the PD-1/PD-L1 axis and merits further development.
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Reference:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics