Published in Org Lett on February 04, 2011
The Davis-Beirut reaction: N1,N2-disubstituted-1H-indazolones via 1,6-electrophilic addition to 3-alkoxy-2H-indazoles. Org Lett (2011) 0.97
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Synthesis of 2H-indazoles by the [3 + 2] cycloaddition of arynes and sydnones. Org Lett (2010) 1.08
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Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension. J Med Chem (2007) 1.06
Synthesis of N2-(substituted benzyl)-3-(4-methylphenyl)indazoles as novel anti-angiogenic agents. Bioorg Med Chem (2005) 1.01
A facile synthesis of new 5H-indazolo[3,2-b]benzo[d]-1,3-oxazines via one-pot intramolecular Bis-heterocyclizations. J Org Chem (2007) 1.01
New antianginal nitro esters with reduced hypotensive activity. Synthesis and pharmacological evaluation of 3-[(nitrooxy)alkyl]-2H-1,3-benzoxazin-4(3H)-ones. J Med Chem (1995) 0.99
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Rapid access to pyrazolo[3,4-c]pyridines via alkyne annulation: limitations of steric control in nickel-catalyzed alkyne insertions. Org Lett (2007) 0.95
Claimed 2,1-benzisoxazoles are indazalones. J Org Chem (2005) 0.91
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection. Bioorg Med Chem Lett (2001) 0.87
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Chemical inhibition of the mitochondrial division dynamin reveals its role in Bax/Bak-dependent mitochondrial outer membrane permeabilization. Dev Cell (2008) 5.67
Loss of tolerance in C57BL/6 mice to the autoantigen E2 subunit of pyruvate dehydrogenase by a xenobiotic with ensuing biliary ductular disease. Hepatology (2008) 2.05
Phenylglycine and sulfonamide correctors of defective delta F508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating. Mol Pharmacol (2005) 1.80
Chemical xenobiotics and mitochondrial autoantigens in primary biliary cirrhosis: identification of antibodies against a common environmental, cosmetic, and food additive, 2-octynoic acid. J Immunol (2005) 1.47
Patients with primary biliary cirrhosis react against a ubiquitous xenobiotic-metabolizing bacterium. Hepatology (2003) 1.46
Identification of 2-nonynoic acid, a cosmetic component, as a potential trigger of primary biliary cirrhosis. J Autoimmun (2006) 1.41
Potent s-cis-locked bithiazole correctors of DeltaF508 cystic fibrosis transmembrane conductance regulator cellular processing for cystic fibrosis therapy. J Med Chem (2008) 1.29
Potent, metabolically stable benzopyrimido-pyrrolo-oxazine-dione (BPO) CFTR inhibitors for polycystic kidney disease. J Med Chem (2011) 1.25
C-O bond formation by polyketide synthases. Science (2002) 1.23
Immunization with a xenobiotic 6-bromohexanoate bovine serum albumin conjugate induces antimitochondrial antibodies. J Immunol (2003) 1.21
4'-Methyl-4,5'-bithiazole-based correctors of defective delta F508-CFTR cellular processing. Bioorg Med Chem Lett (2008) 1.16
Stannous chloride in alcohol: a one-pot conversion of 2-nitro-N-arylbenzamides to 2,3-dihydro-1H-quinazoline-4-ones. J Org Chem (2005) 1.15
Induction of primary biliary cirrhosis in guinea pigs following chemical xenobiotic immunization. J Immunol (2007) 1.12
An oxazolo[3,2-b]indazole route to 1H-indazolones. Org Lett (2009) 1.12
Cyanoquinolines with independent corrector and potentiator activities restore ΔPhe508-cystic fibrosis transmembrane conductance regulator chloride channel function in cystic fibrosis. Mol Pharmacol (2011) 1.07
Oxidative stress caused by pyocyanin impairs CFTR Cl(-) transport in human bronchial epithelial cells. Free Radic Biol Med (2008) 1.05
Pyrazolylthiazole as DeltaF508-cystic fibrosis transmembrane conductance regulator correctors with improved hydrophilicity compared to bithiazoles. J Med Chem (2010) 1.04
CFTR activation in human bronchial epithelial cells by novel benzoflavone and benzimidazolone compounds. Am J Physiol Lung Cell Mol Physiol (2003) 1.03
A facile synthesis of new 5H-indazolo[3,2-b]benzo[d]-1,3-oxazines via one-pot intramolecular Bis-heterocyclizations. J Org Chem (2007) 1.01
N,N-bond-forming heterocyclization: synthesis of 3-alkoxy-2H-indazoles. J Org Chem (2006) 0.98
The Davis-Beirut reaction: N1,N2-disubstituted-1H-indazolones via 1,6-electrophilic addition to 3-alkoxy-2H-indazoles. Org Lett (2011) 0.97
Synthesis of a library of 2-alkyl-3-alkyloxy-2H-indazole-6-carboxamides. J Comb Chem (2007) 0.96
Antimitochondrial antibody heterogeneity and the xenobiotic etiology of primary biliary cirrhosis. Hepatology (2013) 0.96
Nucleophilic substitution of oxazino-/oxazolino-/benzoxazin [3,2-b]indazoles: an effective route to 1H-indazolones. Org Lett (2010) 0.96
Carbodiimide-based benzimidazole library method. J Comb Chem (2006) 0.96
A one-pot-three-step route to triazolotriazepinoindazolones from oxazolino-2H-indazoles. Org Lett (2012) 0.96
A spiroisoxazolinoproline-based amino acid scaffold for solid phase and one-bead-one-compound library synthesis. J Comb Chem (2007) 0.95
Design and synthesis of a hybrid potentiator-corrector agonist of the cystic fibrosis mutant protein DeltaF508-CFTR. Bioorg Med Chem Lett (2009) 0.95
Environment and primary biliary cirrhosis: electrophilic drugs and the induction of AMA. J Autoimmun (2013) 0.95
Highly potent, water soluble benzimidazole antagonist for activated alpha 4 beta 1 integrin. J Med Chem (2007) 0.93
Orthogonally protected thiazole and isoxazole diamino acids: an efficient synthetic route. Chemistry (2010) 0.93
Intramolecular cycloaddition of azomethine ylides in the preparation of pyrrolidino[2',3':3,4]pyrrolidino[1,2- a]benzimidazoles. Org Lett (2007) 0.93
Xenobiotic-induced loss of tolerance in rabbits to the mitochondrial autoantigen of primary biliary cirrhosis is reversible. J Immunol (2004) 0.92
Benzoflavone activators of the cystic fibrosis transmembrane conductance regulator: towards a pharmacophore model for the nucleotide-binding domain. Bioorg Med Chem (2003) 0.92
Claimed 2,1-benzisoxazoles are indazalones. J Org Chem (2005) 0.91
Selective photodynamic therapy by targeted verteporfin delivery to experimental choroidal neovascularization mediated by a homing peptide to vascular endothelial growth factor receptor-2. Arch Ophthalmol (2004) 0.91
Heterocycle-heterocycle strategies: (2-nitrophenyl)isoxazole precursors to 4-aminoquinolines, 1H-indoles, and quinolin-4(1H)-ones. Org Lett (2013) 0.91
Diazocinones: synthesis and conformational analysis. J Org Chem (2006) 0.90
Electrophile-modified lipoic derivatives of PDC-E2 elicits anti-mitochondrial antibody reactivity. J Autoimmun (2011) 0.90
Targeting multiple chorismate-utilizing enzymes with a single inhibitor: validation of a three-stage design. J Med Chem (2010) 0.88
Efficient syntheses of the unknown quinolino[2,3-c]cinnolines; synthesis of neocryptolepines. Org Lett (2010) 0.88
ESIPT-mediated photocycloadditions of 3-hydroxyquinolinones: development of a fluorescence quenching assay for reaction screening. Org Lett (2011) 0.88
Aminodeoxychorismate synthase inhibitors from one-bead one-compound combinatorial libraries: "staged" inhibitor design. J Med Chem (2006) 0.88
Xenobiotics and autoimmunity: does acetaminophen cause primary biliary cirrhosis? Trends Mol Med (2012) 0.88
OBOC small-molecule combinatorial library encoded by halogenated mass-tags. Org Lett (2004) 0.87
Comparison of solid-phase and solution-phase chiral auxiliaries in the alkylation/iodolactonization sequence to gamma-butyrolactones. J Org Chem (2002) 0.87
Synthesis of spiro-fused pyrazolidoylisoxazolines. J Org Chem (2011) 0.87
Isoxazolodihydropyridinones: 1,3-dipolar cycloaddition of nitrile oxides onto 2,4-dioxopiperidines. ACS Comb Sci (2012) 0.87
Design and synthesis of propeller-shaped dispiroisoxazolinopiperidinochromanones. J Comb Chem (2008) 0.86
Structure-activity relationships of cyanoquinolines with corrector-potentiator activity in ΔF508 cystic fibrosis transmembrane conductance regulator protein. J Med Chem (2012) 0.86
Autoreactivity to lipoate and a conjugated form of lipoate in primary biliary cirrhosis. Gastroenterology (2003) 0.86
Quinoxaline 1,4-dioxides are novel angiogenesis inhibitors that potentiate antitumor effects of ionizing radiation. Int J Oncol (2004) 0.86
A novel route to fully substituted 1H-pyrazoles. J Org Chem (2005) 0.85
Parallel Synthesis of bis-heterocyclic isoxazolylmethyl- and isoxazolinylmethylpyrazoles. J Comb Chem (2010) 0.85
One-pot, two-step cascade synthesis of quinazolinotriazolobenzodiazepines. Org Lett (2012) 0.84
7-Substituted 8-aza-7-deazaadenosines for modification of the siRNA major groove. Org Biomol Chem (2012) 0.83
Facile synthesis of glycosylated Fmoc amino acid building blocks assisted by microwave irradiation. Carbohydr Res (2010) 0.83
Asymmetric catalysis: resin-bound hydroxyprolylthreonine derivatives in enamine-mediated reactions. Angew Chem Int Ed Engl (2008) 0.83
Selectively targeting T- and B-cell lymphomas: a benzothiazole antagonist of alpha4beta1 integrin. J Med Chem (2009) 0.83
Selective nucleophilic chemistry in the synthesis of 5-carbamoyl-3-sulfanylmethylisoxazole-4-carboxylic acids. J Comb Chem (2007) 0.83
Antimitochondrial antibody recognition and structural integrity of the inner lipoyl domain of the E2 subunit of pyruvate dehydrogenase complex. J Immunol (2013) 0.82
The radiosensitizer 2-benzoyl-3-phenyl-6,7-dichloroquinoxaline 1,4-dioxide induces DNA damage in EMT-6 mammary carcinoma cells. Radiat Oncol (2009) 0.82
Microwave-mediated heterocyclization to benzimidazo[2,1-b]quinazolin-12(5H)-ones. J Org Chem (2007) 0.82
Quinoxaline 1,4-dioxides: hypoxia-selective therapeutic agents. Mol Carcinog (2002) 0.82
Isoxazolopyrimidines as Novel ΔF508-CFTR Correctors. Synlett (2010) 0.82
Multicomponent assembly of highly substituted indoles by dual palladium-catalyzed coupling reactions. Angew Chem Int Ed Engl (2012) 0.82
3-(2-Benzyloxyphenyl)isoxazoles and isoxazolines: synthesis and evaluation as CFTR activators. Bioorg Med Chem Lett (2003) 0.82
Microwave-assisted synthesis of 3-nitroindoles from N-aryl enamines via intramolecular arene-alkene coupling. Org Lett (2012) 0.81
Halogenated benzimidazole carboxamides target integrin alpha4beta1 on T-cell and B-cell lymphomas. Cancer Res (2010) 0.80
The quinoxaline di-N-oxide DCQ blocks breast cancer metastasis in vitro and in vivo by targeting the hypoxia inducible factor-1 pathway. Mol Cancer (2014) 0.80
Versatile "traceless" sulfone linker for SPOS: preparation of isoxazolinopyrrole 2-carboxylates. J Org Chem (2002) 0.80
Multicomponent macrocyclization reactions (MCMRs) employing highly reactive acyl ketene and nitrile oxide intermediates. Org Lett (2011) 0.80
Quinoxalino[2,3-c]cinnolines and their 5-N-oxide: alkoxylation of methyl-substituted quinoxalino[2,3-c]cinnolines to acetals and orthoesters. J Org Chem (2011) 0.80
Functional fluorescently labeled bithiazole ΔF508-CFTR corrector imaged in whole body slices in mice. Bioconjug Chem (2011) 0.80
ABSOLUTE CONFIGURATION AND BIOLOGICAL PROPERTIES OF ENANTIOMERS OF CFTR INHIBITOR BPO-27. ACS Med Chem Lett (2013) 0.79
Facile one-pot assembly of imidazotriazolobenzodiazepines via indium(III)-catalyzed multicomponent reactions. Org Lett (2013) 0.79
A library of 3-aryl-4,5-dihydroisoxazole-5-carboxamides. J Comb Chem (2007) 0.79
The Davis-Beirut Reaction: a novel entry into 2H-indazoles and indazolones. Recent biological activity of indazoles. Mini Rev Med Chem (2012) 0.79
Sulfamoyl-4-oxoquinoline-3-carboxamides: novel potentiators of defective DeltaF508-cystic fibrosis transmembrane conductance regulator chloride channel gating. Bioorg Med Chem Lett (2005) 0.79
Controlling Selectivity for Cycloadditions of Nitrones and Alkenes Tethered by Benzimidazoles: Combining Experiment and Theory. European J Org Chem (2009) 0.79
Constrained bithiazoles: small molecule correctors of defective ΔF508-CFTR protein trafficking. J Med Chem (2014) 0.78
Click-based synthesis of triazolobithiazole ΔF508-CFTR correctors for cystic fibrosis. Bioorg Med Chem (2012) 0.78
Expedient synthesis of a 72-membered isoxazolino-β-ketoamide library by a 2·3-component reaction. ACS Comb Sci (2012) 0.78
Synthesis of thiazolo- and 7,8-dihydrothiazolo[4,5-e]benzoisoxazoles. J Comb Chem (2009) 0.78
Synthesis and biological activity of 2-(4,5-dihydroisoxazol-5-yl)-1,3,4-oxadiazoles. Bioorg Med Chem Lett (2009) 0.78
Acid and base catalyzed Davis-Beirut reaction: experimental and theoretical mechanistic studies and synthesis of novel 3-amino-2H-indazoles. Tetrahedron Lett (2012) 0.78
Mechanisms for formation of diazocinones, pyridazines, and pyrazolines from tetrazines--oxyanion-accelerated pericyclic cascades? J Org Chem (2009) 0.77