A first-in-human study of AMG 208, an oral MET inhibitor, in adult patients with advanced solid tumors. [PDF]
, 2015 BackgroundThis first-in-human study evaluated AMG 208, a small-molecule MET inhibitor, in patients with advanced solid tumors.MethodsThree to nine patients were enrolled into one of seven AMG 208 dose cohorts (25, 50, 100, 150, 200, 300, and 400 mg ...
Amore, Benny +14 more
core +6 more sources
Synthesis of Novel N1 and N2 Indazole Derivatives
E-Journal of Chemistry, 2012 The alkylation of 5-cyano indazoles 2 in the presence of readily available imidizolium salts (ionic liquids) (Bmim)BF4 as phase transfer catalyst were performed to afford the regio isomers N1-and N2-(substituted alkyl)-5-cyano indazoles. The N1-alkylated
Prasanna Bethanamudi +4 more
doaj +1 more source
Estrogen Receptor Transrepresses Brain Inflammation [PDF]
, 2011 Estrogen receptors (ERs) have long been implicated in the etiology of multiple sclerosis, but no clear molecular mechanisms have linked ERs to the disease's pathology. Now Saijo et al.
Gosselin, David, Rivest, Serge
core +1 more source
Crystal structure of 4-(benzofuran-2-yl)-2-(3-(4-fluorophenyl)-3,3a,4,5-tetrahydro-2H-benzo[g]indazol-2-yl)thiazole, C28H20FN3OS [PDF]
, 2016 C28H20FN3OS, triclinic, P1̅ (no. 2), a = 9.5719(5) Å, b = 10.7499(6) Å, c = 10.9238(5) Å, α = 95.470(4)°, β = 102.133(4)°, γ = 97.962(4)°, V = 1079.30(10) Å3, R gt(F) = 0.0482, wR ref(F 2) = 0 ...
Abdel-Wahab, Bakr F. +4 more
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Hg(II) Complexes Constructed from Indazole Ligands as New Heterogeneous Catalyst for the Biginelli/Transesterification Reaction: Synthesis and Quantum-Chemical Investigations [PDF]
Iranian Journal of Chemistry & Chemical Engineering, 2022 The present work deals with the synthesis, spectral characterization, DFT calculations, and catalytic activity of the new Hg(II) complexes derived from indazole ligands. The o-amino-ketones were obtained from the reduction of 6H-isoxazolo[4,3-e]indazoles
Elaheh Alikhani +3 more
doaj +1 more source
7-Nitro indazole, an inhibitor of neuronal nitric oxide synthase, attenuates pilocarpine-induced seizures [PDF]
, 1995 7-Nitro indazole (25–100 mg/kg i.p.), an inhibitor of neuronal nitric oxide (NO) synthase, attenuated the severity of pilocarpine (300 mg/kg i.p.)-induced seizures in mice. This indicates that the decreased neuroexcitability of the central nervous system
Dzoljic, E. (Eleonora) +2 more
core +1 more source
Angewandte Chemie, EarlyView.We present a new class of electronically and sterically hindered N‐heterocyclic carbenes, referred to as bridged cyclic (amino)ylide carbene (bCAYC), where 9H‐pyrrolo[1,2‐a]indole acted as carbene core and diaryl sulfonium as ylide partner. Corresponding bCAYC‐Au(I) exhibits a weak secondary intramolecular Au···H−C(sp3) interaction as a secondary ...
Sourav Sekhar Bera +6 more
wiley +2 more sources
One-Pot Synthesis of Novel 2,3-Dihydro-1H-indazoles
Molecules, 2011 A copper(I)-mediated one-pot synthesis of 2,3-dihydro-1H-indazole heterocycles has been developed. This synthetic route provides the desired indazoles in moderate to good yields (55%–72%) which are substantially better than those achievable with an ...
Antonio J. Lepore, Gary W. Breton
doaj +1 more source
Regiospecific synthesis of N2-aryl 1,2,3-triazoles from 2,5-disubstituted tetrazoles via photochemically generated nitrile imine intermediates [PDF]
, 2014 The synthesis of N2-aryl 1,2,3-triazoles from 2,5-disubstituted tetrazoles was achieved under photochemical conditions. This simple and mild one-step reaction provides regiospecific access to 2,4,5-substituted 1,2,3-triazoles via a nitrile imine ...
Harris, Robert +2 more
core +1 more source
Photoenzymatic Hydroalkylation Enables Streamlined Access to Aryl Glutarimide Precursors
Angewandte Chemie, EarlyView.We report a photoenzymatic hydroalkylation that enables streamlined, stereocontrolled access to aryl glutarimide precursors relevant to targeted protein degradation. Engineered flavin‐dependent “ene”‐reductases provide broad scope and high enantioselectivity through a distinct electron transfer–enantioselective proton transfer pathway.
Zhi Xu +9 more
wiley +2 more sources