Design and synthesis of an activity-based protein profiling probe derived from cinnamic hydroxamic acid.
Basic Information
ID: ALA3751715
Journal: Bioorg Med Chem
Title: Design and synthesis of an activity-based protein profiling probe derived from cinnamic hydroxamic acid.
Authors: Ai T, Qiu L, Xie J, Geraghty RJ, Chen L.
Abstract: In our continued effort to discover new anti-hepatitis C virus (HCV) agents, we validated the anti-replicon activity of compound 1, a potent and selective anti-HCV hydroxamic acid recently reported by us. Generally favorable physicochemical and in vitro absorption, distribution, metabolism, and excretion (ADME) properties exhibited by 1 made it an ideal parent compound from which activity-based protein profiling (ABPP) probe 3 was designed and synthesized. Evaluation of probe 3 revealed that it possessed necessary anti-HCV activity and selectivity. Therefore, we have successfully obtained compound 3 as a suitable ABPP probe to identify potential molecular targets of compound 1. Probe 3 and its improved analogs are expected to join a growing list of ABPP probes that have made important contributions to not only the studies of biochemical and cellular functions but also discovery of selective inhibitors of protein targets.
CiteXplore: 26753813
DOI: 10.1016/j.bmc.2015.12.035
Patent ID: ┄