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10.1021/ja512112j http://scihub22266oqcxt.onion/10.1021/ja512112j C4386841!4386841 !25697265     free     free     free Warning: file_get_contents(https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&id=25697265 &cmd=llinks): Failed to open stream: HTTP request failed! 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Design, synthesis, and protein crystallography of biaryltriazoles as potent tautomerase inhibitors of macrophage migration inhibitory factor |pdf=|usr=}}{{25697265 }} gab.com Text Design, synthesis, and protein crystallography of biaryltriazoles as potent tautomerase inhibitors of macrophage migration inhibitory factor JO: J Am Chem Soc http://www.kidney.de/pget.php?&tw=1&pmid=25697265 #FOAvip Optimization is reported for biaryltriazoles as inhibitors of the tautomerase activity of human macrophage migration inhibitory factor (MIF), a proinflammatory cytokine associated with numerous inflammatory diseases and cancer. A combined approach was taken featuring organic synthesis, enzymatic assaying, crystallography, and modeling including free-energy perturbation (FEP) calculations. X-ray crystal structures for 3a and 3b bound to MIF are reported and provided a basis for the modeling efforts. The accommodation of the inhibitors in the binding site is striking with multiple hydrogen bonds and aryl-aryl interactions. Additional modeling encouraged pursuit of 5-phenoxyquinolinyl analogues, which led to the very potent compound 3s. Activity was further enhanced by addition of a fluorine atom adjacent to the phenolic hydroxyl group as in 3w, 3z, 3aa, and 3bb to strengthen a key hydrogen bond. It is also shown that physical properties of the compounds can be modulated by variation of solvent-exposed substituents. Several of the compounds are likely the most potent known MIF tautomerase inhibitors; the most active ones are more than 1000-fold more active than the well-studied (R)-ISO-1 and more than 200-fold more active than the chromen-4-one Orita-13. Twit Text FOAVip Design, synthesis, and protein crystallography of biaryltriazoles as potent tautomerase inhibitors of macrophage migration inhibitory factor ????J Am Chem Soc http://www.kidney.de/pget.php?&tw=1&pmid=25697265 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=25697265 #FOAvip English Wikipedia <ref>{{Cite pmid|25697265 }}</ref> Design, synthesis, and protein crystallography of biaryltriazoles as potent tautomerase inhibitors of macrophage migration inhibitory factor #MMPMID25697265 Dziedzic P ; Cisneros JA ; Robertson MJ ; Hare AA ; Danford NE ; Baxter RH ; Jorgensen WL J Am Chem Soc 2015[Mar]; 137 (8 ): 2996-3003 PMID25697265 show ga Optimization is reported for biaryltriazoles as inhibitors of the tautomerase activity of human macrophage migration inhibitory factor (MIF), a proinflammatory cytokine associated with numerous inflammatory diseases and cancer. A combined approach was taken featuring organic synthesis, enzymatic assaying, crystallography, and modeling including free-energy perturbation (FEP) calculations. X-ray crystal structures for 3a and 3b bound to MIF are reported and provided a basis for the modeling efforts. The accommodation of the inhibitors in the binding site is striking with multiple hydrogen bonds and aryl-aryl interactions. Additional modeling encouraged pursuit of 5-phenoxyquinolinyl analogues, which led to the very potent compound 3s. Activity was further enhanced by addition of a fluorine atom adjacent to the phenolic hydroxyl group as in 3w, 3z, 3aa, and 3bb to strengthen a key hydrogen bond. It is also shown that physical properties of the compounds can be modulated by variation of solvent-exposed substituents. Several of the compounds are likely the most potent known MIF tautomerase inhibitors; the most active ones are more than 1000-fold more active than the well-studied (R)-ISO-1 and more than 200-fold more active than the chromen-4-one Orita-13. |*Drug Design [MESH] |Chemistry Techniques, Synthetic [MESH] |Crystallography, X-Ray [MESH] |Enzyme Inhibitors/*chemical synthesis/chemistry/*pharmacology [MESH] |Humans [MESH] |Hydrogen Bonding [MESH] |Intramolecular Oxidoreductases/*antagonists & inhibitors/*chemistry [MESH] |Macrophage Migration-Inhibitory Factors/*antagonists & inhibitors/*chemistry [MESH] |Models, Molecular [MESH] |Protein Conformation [MESH] |Solubility [MESH] |Structure-Activity Relationship [MESH] |Triazoles/*chemical synthesis/chemistry/*pharmacology [MESH]Design, synthesis, and protein crystallography of biaryltriazoles as p(epmc).pdf DeepDyve Pubget Overpricing