Shergalis, Andrea; Xue, Ding; Gharbia, Fatma Z.; Driks, Hannah; Shrestha, Binita; Tanweer, Amina; Cromer, Kirin; Ljungman, Mats; Neamati, Nouri published the artcile< Characterization of Aminobenzylphenols as Protein Disulfide Isomerase Inhibitors in Glioblastoma Cell Lines>, Synthetic Route of 198904-53-9, the main research area is aminobenzylphenol structure screening preparation PDIA1 inhibitor glioblastoma.
Disulfide bond formation is a critical post-translational modification of newly synthesized polypeptides in the oxidizing environment of the endoplasmic reticulum and is mediated by protein disulfide isomerase (PDIA1). In this study, we report a series of α-aminobenzylphenol analogs as potent PDI inhibitors. The lead compound, AS15, is a covalent nanomolar inhibitor of PDI, and the combination of AS15 analogs with glutathione synthesis inhibitor buthionine sulfoximine (BSO) leads to synergistic cell growth inhibition. Using nascent RNA sequencing, we show that an AS15 analog triggers the unfolded protein response in glioblastoma cells. A BODIPY-labeled analog binds proteins including PDIA1, suggesting that the compounds are cell-permeable and reach the intended target. Taken together, these findings demonstrate an extensive biochem. characterization of a novel series of highly potent reactive small mols. that covalently bind to PDI.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 198904-53-9 belongs to class thiazole, and the molecular formula is C10H7NOS, Synthetic Route of 198904-53-9.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica