An efficient reduction of hexavalent chromium [Cr(VI)] induced by gaseous glow discharge plasma (GDP) generated between a pointed platinum anode and the surface of an aqueous solution has been achieved for the first time. Experimental results show that Cr(VI) could be smoothly reduced to trivalent state [Cr(III)] by using GDP with 500 V as the optimum operating voltage. The rate of Cr(VI) reduction was enhanced by either decreasing the solution pH or adding radical scavengers to the solution. At initial pH 2.0, 100 mg/L of Cr(VI) was completely reduced within 10 min of GDP treatment in the presence of 100 mg/L phenol. A possible reaction mechanism was proposed based on the reduction kinetics. Energy efficiency of Cr(VI) reduction in GDP was compared with that in other competitive processes.
Macrocycles have attracted significant attention in drug discovery recently. In fact, a few de novo designed macrocyclic kinases inhibitors are currently in clinical trials with good potency and selectivity for their intended target. In this paper, we have successfully engaged a structure-based drug design approach to discover macrocyclic pyrimidines as potent Mer tyrosine kinase (MerTK)-specific inhibitors. An enzyme-linked immunosorbent assay (ELISA) in a 384-well format was employed to evaluate the inhibitory activity of macrocycles in a cell-based assay assessing tyrosine phosphorylation of MerTK. Through SAR studies, analogue 11 (UNC2541) was identified as a potent and MerTK-specific inhibitor and exhibits sub-micro molar inhibitory activity in the cell-based ELISA assay. In addition, an X-ray structure of MerTK protein in complex with 11 was resolved to show that these macro-cycles bind in the MerTK ATP pocket.
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