A sensitive assay for the determination of E7090, a novel selective inhibitor of fibroblast growth factor receptors, and its metabolite in human plasma by UPLC-MS/MS with at-column dilution.

E7090, a novel fibroblast growth factor receptors inhibitor, is currently under clinical development for the treatment of patients with solid tumors. The previous assay was insufficient in detection sensitivity for E7090 and high exposure of a dealkylated metabolite, M2, was noted in a clinical trial at low doses. Thus, a sensitive assay for the simultaneous determination of E7090 and M2 in human plasma has been developed using ultra-performance liquid chromatography with tandem mass spectrometer (UPLC-MS/MS).

Detection of Thiol Functionality and Disulfide Bond Formation by Polyoxometalate.

The detection of thiol functionality and intramolecular disulfide bond formation of peptides using the α-Keggin type polyoxometalate molybdenum-oxygen cluster (HPMoO·HO) is described. Our method entails the addition of this polyoxometalate to solutions of thiol, whereupon the color of the solution changes from colorless to deep blue. Reduction of the polyoxometalate from Mo(VI) to Mo(V) occurs with concomitant oxidation of the thiol functionality, to form disulfide bonds.

Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor.

Synthesis and evaluation of new scaffold phenylisoserine derivatives connected with the essential functional groups against SARS CoV 3CL protease are described. The phenylisoserine backbone was found by simulation on GOLD software and the structure activity relationship study of phenylisoserine derivatives gave SK80 with an IC value of 43μM against SARS CoV 3CL R188I mutant protease.