92829-67-9Relevant academic research and scientific papers
Synthesis of Functionalized 2-(4-Hydroxyphenyl)-3-methylbenzofuran Allosteric Modulators of Hsp90 Activity
Sattin, Sara,Panza, Matteo,Vasile, Francesca,Berni, Francesca,Goti, Giulio,Tao, Jiahui,Moroni, Elisabetta,Agard, David,Colombo, Giorgio,Bernardi, Anna
supporting information, p. 3349 - 3364 (2016/07/26)
Hsp90 is a molecular chaperone that plays a pivotal role in the cell life cycle. ATP-regulated internal dynamics are critical to Hsp90 function and we recently demonstrated that these dynamics can be modulated in an allosteric fashion; the protein C-terminal domain (CTD) can be effectively targeted with a family of 2-phenyl-benzofuran derivatives. Here we describe the expansion of the initial library, reporting 28 new derivatives that explore the chemical space at opposite ends of the benzofuran scaffold. Interactions of the compounds with a full-length protein homolog were explored by Saturation Transfer Difference (STD) NMR spectroscopy. In this context we also report the interaction epitope of Novobiocin, a known CTD inhibitor.
NOVEL VASCULAR LEAKAGEAGE INHIBITOR
-
, (2015/01/07)
The present disclosure relates to a novel vascular leakage inhibitor. The novel vascular leakage inhibitor of the present invention inhibits the apoptosis of vascular endothelial cells, inhibits the formation of actin stress fibers induced by VEGF, and enhances the cortical actin ring structure, thereby inhibiting vascular leakage. Accordingly, the vascular leakage inhibitor of the present invention can prevent or treat various diseases caused by vascular leakage. Since the vascular leakage inhibitor of the present invention is synthesized from commercially available or easily synthesizable pregnenolones, it has remarkably superior feasibility of commercial synthesis.
Selective Ligands for the Neuronal Nicotinic Receptors and Uses Thereof
-
Page/Page column 27, (2009/12/04)
The present application describes selective ligands of formula (I) for neuronal nicotinic receptors (NNRs), more specifically for the α4β2 NNR subtype, compositions thereof, and methods of using the same, wherein X, R1, X, R2, R3, L1, m, n, p, and q are defined in the specification.
4-SUBSTITUTED AZAADAMANTANE DERIVATIVES AND METHODS OF USE THEREOF
-
Page/Page column 33, (2008/12/04)
The invention relates to compounds that are 4-substituted azaadamantane derivatives, compositions comprising such compounds, and methods of using such compounds and compositions.
Control of parasites in animals by the use of novel trifluoromethanesulfonanilide oxime ether derivatives
-
Page/Page column 28, (2010/10/20)
Novel trifluoromethanesulfonanilide oxime ether compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo or ex vivo.
Synthesis and pharmacological evaluation of benzofuran-acetamides as 'antineophobic' mitochondrial DBI receptor complex ligands
Liao, Yi,Kozikowski, Alan P.,Guidotti, Alessandro,Costa, Erminio
, p. 2099 - 2102 (2007/10/03)
A series of novel benzofuran analogues of N,N-di-n-hexyl-2- phenylindole-3-acetamide (5, FGIN-1-27), a potent and highly specific mitochondrial DBI receptor complex ligand, were synthesized by a modified Fischer method and found in vitro and in vivo to be equally potent and selective as FGIN-1-27.
Nucleophilic Aromatic Substitution on Tricarbonyl(halogenoarene)chromium Complexes: A New Synthesis of O-Arylhydroxylamines
Baldoli, Clara,Buttero, Paola Del,Licandro, Emanuela,Maiorana, Stefano
, p. 344 - 345 (2007/10/02)
A series of O-arylhydroxylamines 4 have been synthesized under mild conditions and in good yields by the reaction of tricarbonyl(halogenoarene)chromium complexes 1 with N-(tert-butyloxycarbonyl)hydroxylamine (tert-butyl N-hydroxycarbamate), followed by decomplexation and acidic hydrolysis of the tert-butyl N-(aryloxy)carbamates 3.
