Published in Drug Metab Dispos on December 11, 2013
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An alkoxide-directed intermolecular [2+2+1] annulation: a three-component coupling reaction for the synthesis of tetrasubstituted alpha,beta-unsaturated gamma-lactams. Angew Chem Int Ed Engl (2007) 1.57
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Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis. Cancer Res (2013) 1.46
Synthesis of conolidine, a potent non-opioid analgesic for tonic and persistent pain. Nat Chem (2011) 1.44
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Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist. ACS Chem Biol (2010) 1.22
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Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ. ACS Chem Biol (2010) 1.14
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Total synthesis and structure elucidation of (+)-phorbasin C. J Am Chem Soc (2009) 1.06
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Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance(). Medchemcomm (2012) 1.05
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Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos (2012) 1.04
Conversion of allylic alcohols to stereodefined trisubstituted alkenes: a complementary process to the Claisen rearrangement. J Am Chem Soc (2008) 1.03
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Chemical and computational methods for the characterization of covalent reactive groups for the prospective design of irreversible inhibitors. J Med Chem (2014) 1.01
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Convergent and stereodivergent synthesis of complex 1-aza-7-oxabicyclo[2.2.1]heptanes. J Am Chem Soc (2011) 0.99
Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity. J Med Chem (2010) 0.98
Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J Med Chem (2008) 0.97
Validation of isolated metabolites from drug metabolism studies as analytical standards by quantitative NMR. Drug Metab Dispos (2010) 0.97
Metallacycle-Mediated Cross-Coupling with Substituted and Electronically Unactivated Alkenes. Chem Sci (2011) 0.97
Immune-mediated agranulocytosis caused by the cocaine adulterant levamisole: a case for reactive metabolite(s) involvement. Drug Metab Dispos (2012) 0.96
Characterization of dasatinib and its structural analogs as CYP3A4 mechanism-based inactivators and the proposed bioactivation pathways. Drug Metab Dispos (2009) 0.96
Small Molecule c-jun-N-terminal Kinase (JNK) Inhibitors Protect Dopaminergic Neurons in a Model of Parkinson's Disease. ACS Chem Neurosci (2011) 0.96
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Construction of highly functionalized medium-sized rings: synthesis of hyperforin and perforatumone model systems. Angew Chem Int Ed Engl (2005) 0.96
Convergent synthesis of stereodefined exo-alkylidene-gamma-lactams from beta-halo allylic alcohols. Org Lett (2009) 0.96
Studies in macrolide antibiotic synthesis: the role of tethered alkoxides in titanium alkoxide-mediated regioselective reductive coupling reactions. Org Lett (2006) 0.94
Total synthesis of lehualide B by allylic alcohol-alkyne reductive cross-coupling. J Am Chem Soc (2010) 0.94
Highly selective inhibition of human CYP3Aa in vitro by azamulin and evidence that inhibition is irreversible. Drug Metab Dispos (2004) 0.94
Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett (2013) 0.93
Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos (2012) 0.93
An annulation reaction for the synthesis of cross-conjugated triene-containing hydroindanes from acyclic precursors. Org Lett (2014) 0.92
Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs. Drug Metab Dispos (2012) 0.92
JNK Inhibition Protects Dopamine Neurons and Provides Behavioral Improvement in a Rat 6-hydroxydopamine Model of Parkinson's Disease. ACS Chem Neurosci (2011) 0.91
Chemoselective reductive cross-coupling of 1,5-diene-3-ols with alkynes: a facile entry to stereodefined skipped trienes. J Am Chem Soc (2010) 0.91
Evaluating genetic markers and neurobiochemical analytes for fluoxetine response using a panel of mouse inbred strains. Psychopharmacology (Berl) (2011) 0.90
In vitro metabolism and covalent binding of enol-carboxamide derivatives and anti-inflammatory agents sudoxicam and meloxicam: insights into the hepatotoxicity of sudoxicam. Chem Res Toxicol (2008) 0.90
Identification, design and biological evaluation of bisaryl quinolones targeting Plasmodium falciparum type II NADH:quinone oxidoreductase (PfNDH2). J Med Chem (2012) 0.90
Carbon monoxide poisoning is prevented by the energy costs of conformational changes in gas-binding haemproteins. Proc Natl Acad Sci U S A (2011) 0.90
Decoding split and pool combinatorial libraries with electron-transfer dissociation tandem mass spectrometry. J Am Soc Mass Spectrom (2013) 0.89
Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents. J Med Chem (2013) 0.89
Bioactivation of the epidermal growth factor receptor inhibitor gefitinib: implications for pulmonary and hepatic toxicities. Chem Res Toxicol (2009) 0.89
Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol (2003) 0.89
Total synthesis of callystatin a by titanium-mediated reductive alkyne-alkyne cross-coupling. Angew Chem Int Ed Engl (2008) 0.89
Three-component coupling sequence for the regiospecific synthesis of substituted pyridines. J Am Chem Soc (2011) 0.89
Group 4 metals in polyketide synthesis: a convergent strategy for the synthesis of polypropionate-derived (E,E)-trisubstituted 1,3-dienes. Org Lett (2005) 0.88
Prevalence of extended spectrum beta lactamase and AmpC beta lactamase producers among Escherichia coli isolates in a tertiary care hospital in Jaipur. Indian J Pathol Microbiol (2008) 0.88
4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency. J Med Chem (2014) 0.88
The pharmacokinetics, metabolism, and clearance mechanisms of tofacitinib, a janus kinase inhibitor, in humans. Drug Metab Dispos (2014) 0.87
Total synthesis of macbecin I. Angew Chem Int Ed Engl (2008) 0.87
Identification of a novel non-retinoid pan inverse agonist of the retinoic acid receptors. ACS Chem Biol (2011) 0.87
Thiazolides as novel antiviral agents. 2. Inhibition of hepatitis C virus replication. J Med Chem (2011) 0.87
Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors. Bioorg Med Chem Lett (2011) 0.87
Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival. ACS Chem Biol (2015) 0.87
Polyketide assembly by alkene-alkyne reductive cross-coupling: spiroketals through the union of homoallylic alcohols. J Am Chem Soc (2010) 0.86
D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. ACS Med Chem Lett (2012) 0.86
Convergent synthesis of piperidines by the union of conjugated alkynes with imines: a unique regioselective bond construction for heterocycle synthesis. Org Lett (2009) 0.86
Metabolism considerations for kinase inhibitors in cancer treatment. Expert Opin Drug Metab Toxicol (2010) 0.86
Demonstration of the innate electrophilicity of 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine (BETP), a small-molecule positive allosteric modulator of the glucagon-like peptide-1 receptor. Drug Metab Dispos (2013) 0.86
Chroman-3-amides as potent Rho kinase inhibitors. Bioorg Med Chem Lett (2008) 0.85
Enantio- and diastereoselective synthesis of cyclic beta-hydroxy allylsilanes via sequential aldehyde gamma-silylallylboration and ring-closing metathesis reactions. Org Lett (2003) 0.85
Comparison of in vitro metabolism of ticlopidine by human cytochrome P450 2B6 and rabbit cytochrome P450 2B4. Drug Metab Dispos (2010) 0.84
Metabolism, excretion and pharmacokinetics of [14C]crizotinib following oral administration to healthy subjects. Xenobiotica (2014) 0.84
Mechanism-based inactivation of cytochrome P450 2D6 by 1-[(2-ethyl-4-methyl-1H-imidazol-5-yl)methyl]- 4-[4-(trifluoromethyl)-2-pyridinyl]piperazine: kinetic characterization and evidence for apoprotein adduction. Chem Res Toxicol (2004) 0.84
Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors. J Med Chem (2010) 0.84
Cytochrome P450-mediated bioactivation of the epidermal growth factor receptor inhibitor erlotinib to a reactive electrophile. Drug Metab Dispos (2010) 0.84
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Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats. Bioorg Med Chem Lett (2010) 0.83
Metformin represses drug-induced expression of CYP2B6 by modulating the constitutive androstane receptor signaling. Mol Pharmacol (2013) 0.83
Inhibitors of PIM-1 kinase: a computational analysis of the binding free energies of a range of imidazo [1,2-b] pyridazines. J Chem Inf Model (2010) 0.83
Synthesis of benzoquinone ansamycin-inspired macrocyclic lactams from shikimic acid. Angew Chem Int Ed Engl (2013) 0.83