Lu, Min; Zhang, Hongjun; Li, Derun; Childers, Matthew; Pu, Qinglin; Palte, Rachel L.; Gathiaka, Symon; Lyons, Thomas W.; Palani, Anandan; Fan, Peter W.; Spacciapoli, Peter; Miller, J. Richard; Cho, Hyelim; Cheng, Mangeng; Chakravarthy, Kalyan; O′Neil, Jennifer; Eangoor, Padmanabhan; Beard, Adam; Kim, Hai-Young; Sauri, Josep; Gunaydin, Hakan; Sloman, David L.; Siliphaivanh, Phieng; Cumming, Jared; Fischer, Christian published the artcile< Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology>, Quality Control of 53636-56-9, the main research area is proline arginase inhibitor oral bioavailability immuno oncol.
Recent data suggest that the inhibition of arginase (ARG) has therapeutic potential for the treatment of a number of indications ranging from pulmonary and vascular disease to cancer. Thus, high demand exists for selective small mol. ARG inhibitors with favorable druglike properties and good oral bioavailability. In light of the significant challenges associated with the unique physicochem. properties of previously disclosed ARG inhibitors, we use structure-based drug design combined with a focused optimization strategy to discover a class of boronic acids featuring a privileged proline scaffold with superior potency and oral bioavailability. These compounds, exemplified by inhibitors 4a, 18, and 27, demonstrated a favorable overall profile, and 4a was well tolerated following multiple days of dosing at concentrations that exceed those required for serum arginase inhibition and concomitant arginine elevation in a syngeneic mouse carcinoma model.
ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 53636-56-9 belongs to class pyridine-derivatives, and the molecular formula is C7H6BrNO2, Quality Control of 53636-56-9.