Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 2-Chloronicotinoyl chloride, is researched, Molecular C6H3Cl2NO, CAS is 49609-84-9, about Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells.Recommanded Product: 2-Chloronicotinoyl chloride.
Sodium taurocholate cotransport polypeptide (NTCP) plays an important role in the development of hepatitis and acts as a switch to allow hepatitis virus to enter hepatic cells. As the entry receptor protein of hepatitis virus, NTCP is also an effective target for the treatment of hepatocellular carcinoma. Herein, twenty-five benzamide analogs were synthesized based on the virtual screening design and their anti-proliferative activities against HepG2 cells were evaluated in vitro. Compound I was found to be promising, with an IC50 value of 2.8μM. The apoptosis induced by I was characterized by the regulation of markers, including an increase in Bax, cleaved-caspase 3, and cleaved-PARP proteins, and a decrease in Bcl-2 protein. Mol. docking and mol. dynamics (MD) simulation confirmed that compound I can bind tightly to NTCP. Western blot anal. also showed that NTCP was inhibited. Altogether, these results indicate that compound I acts as a novel NTCP inhibitor to induce apoptosis in HepG2 cells.
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Phosphine ligand,
Chiral phosphine ligands in asymmetric synthesis. Molecular structure and absolute configuration of (1,5-cyclooctadiene)-(2S,3S)-2,3-bis(diphenylphosphino)butanerhodium(I) perchlorate tetrahydrofuran solvate