223707-22-0Relevant articles and documents
Identification and characterization of novel benzil (diphenylethane-1,2- dione) analogues as inhibitors of mammalian carboxylesterases
Wadkins, Randy M.,Hyatt, Janice L.,Wei, Xin,Yoon, Kyoung Jin P.,Wierdl, Monika,Edwards, Carol C.,Morton, Christopher L.,Obenauer, John C.,Damodaran, Komath,Beroza, Paul,Danks, Mary K.,Potter, Philip M.
, p. 2906 - 2915 (2005)
Carboxylesterases (CE) are ubiquitous enzymes responsible for the metabolism of xenobiotics. Because the structural and amino acid homology among esterases of different classes, the identification of selective inhibitors of these proteins has proved problematic. Using Telik's target-related affinity profiling (TRAP) technology, we have identified a class of compounds based on benzil (1,2-diphenylethane-1,2-dione) that are potent CE inhibitors, with K i values in the low nanomolar range. Benzil and 30 analogues demonstrated selective inhibition of CEs, with no inhibitory activity toward human acetylcholinesterase or butyrylcholinesterase. Analysis of structurally related compounds indicated that the ethane-1,2-dione moiety was essential for enzyme inhibition and that potency was dependent on the presence of, and substitution within, the benzene ring. 3D-QSAR analyses of these benzil analogues for three different mammalian CEs demonstrated excellent correlations of observed versus predicted Ki(r2 > 0.91), with cross-validation coefficients (q2) of 0.9. Overall, these results suggest that selective inhibitors of CEs with potential for use in clinical applications can be designed.
Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils
Hicks, Latorya D.,Hyatt, Janice L.,Moak, Teri,Edwards, Carol C.,Tsurkan, Lyudmila,Wierdl, Monika,Ferreira, Antonio M.,Wadkins, Randy M.,Potter, Philip M.
, p. 3801 - 3817 (2008/02/09)
We have synthesized and assessed the ability of symmetrical fluorobenzoins and fluorobenzils to inhibit mammalian carboxylesterases (CE). The majority of the latter were excellent inhibitors of CEs however unexpectedly, the fluorobenzoins were very good enzyme inhibitors. Positive correlations were seen with the charge on the hydroxyl carbon atom, the carbonyl oxygen, and the Hammett constants for the derived Ki values with the fluorobenzoins.
ORGANOMETALLIC COMPLEX, AND LIGHT-EMITTING ELEMENT AND LIGHT-EMITTNG DEVICE USING THE SAME
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Page/Page column 47, (2010/11/08)
It is an object of the present invention to provide a substance capable of emitting phosphorescence. In addition, it is an object of the present invention to provide a light-emitting element that is excellent in chromaticity. One aspect of the present inv