93007-64-8Relevant academic research and scientific papers
Harnessing the Role of HDAC6 in Idiopathic Pulmonary Fibrosis: Design, Synthesis, Structural Analysis, and Biological Evaluation of Potent Inhibitors
Campiani, Giuseppe,Cavella, Caterina,Osko, Jeremy D.,Brindisi, Margherita,Relitti, Nicola,Brogi, Simone,Saraswati, A. Prasanth,Federico, Stefano,Chemi, Giulia,Maramai, Samuele,Carullo, Gabriele,Jaeger, Benedikt,Carleo, Alfonso,Benedetti, Rosaria,Sarno, Federica,Lamponi, Stefania,Rottoli, Paola,Bargagli, Elena,Bertucci, Carlo,Tedesco, Daniele,Herp, Daniel,Senger, Johanna,Ruberti, Giovina,Saccoccia, Fulvio,Saponara, Simona,Gorelli, Beatrice,Valoti, Massimo,Kennedy, Breándan,Sundaramurthi, Husvinee,Butini, Stefania,Jung, Manfred,Roach, Katy M.,Altucci, Lucia,Bradding, Peter,Christianson, David W.,Gemma, Sandra,Prasse, Antje
, p. 9960 - 9988 (2021/07/31)
Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease characterized by a progressive-fibrosing phenotype. IPF has been associated with aberrant HDAC activities confirmed by our immunohistochemistry studies on HDAC6 overexpression in IPF lung tissues. We herein developed a series of novelhHDAC6 inhibitors, having low inhibitory potency overhHDAC1 andhHDAC8, as potential pharmacological tools for IPF treatment. Their inhibitory potency was combined with lowin vitroandin vivotoxicity. Structural analysis of 6h and structure-activity relationship studies contributed to the optimization of the binding mode of the new molecules. The best-performing analogues were tested for their efficacy in inhibiting fibrotic sphere formation and cell viability, proving their capability in reverting the IPF phenotype. The efficacy of analogue 6h was also determined in a validated human lung model of TGF-β1-dependent fibrogenesis. The results highlighted in this manuscript may pave the way for the identification of first-in-class molecules for the treatment of IPF.
Et3SiH + KO: T Bu provide multiple reactive intermediates that compete in the reactions and rearrangements of benzylnitriles and indolenines
Arokianathar, Jude N.,Clark, Kenneth F.,Dimitrova, Daniela,Leach, Stuart G.,Murphy, John A.,Poole, Darren L.,Smith, Andrew J.
, p. 12364 - 12370 (2020/12/08)
The combination of potassium tert-butoxide and triethylsilane is unusual because it generates multiple different types of reactive intermediates simultaneously that provide access to (i) silyl radical reactions, (ii) hydrogen atom transfer reactions to cl
Single-operation deracemization of 3H-indolines and tetrahydroquinolines enabled by phase separation
Lackner, Aaron D.,Samant, Andrew V.,Toste, F. Dean
, p. 14090 - 14093 (2013/10/21)
The single-operation deracemization of 3H indolines and tetrahydroquinolines is described. An asymmetric redox approach was employed, in which a phosphoric acid catalyst, oxidant, and reductant are present in the reaction mixture. The simultaneous presence of both oxidant and reductant was enabled by phase separation and resulted in the isolation of highly enantioenriched starting materials in high yields.
NOVEL ORGANIC ELECTROLUMINESCENT COMPOUNDS AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME
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Paragraph 109; 110; 111; 112; 149; 150; 151; 152, (2014/01/07)
The present invention relates to novel organic electroluminescent compounds and an organic electroluminescent device containing the same. The organic electroluminescent compounds according to the present invention have high luminescent efficiency and a lo
One-pot synthesis of highly substituted indolines
Liu, Kevin G.,Lo, Jennifer R.,Robichaud, Albert J.
experimental part, p. 573 - 577 (2010/09/05)
A general and convenient one-pot synthesis of highly substituted indolines from arylhydrazines and aldehydes is reported. This synthesis allows introduction of substitution at essentially all positions of the indoline nucleus to achieve significant diversity in this biologically important template.
Oxazoloindoles, Pyrrolo- and Azepino-indoles from 3H-Indole 1-Oxides and Acetylenecarboxylic Esters by Skeletal Rearrangements
Letcher, Roy M.,Sin, Della W. M.,Cheung, Kung-Kai
, p. 939 - 944 (2007/10/02)
3H-Indole N-oxides 3 have been prepared from 3H-indoles 1 by hydride reduction followed by m-chloroperbenzoic acid oxidation.Reaction of 3 with dimethyl acetylenedicarboxylate (DMAD) and with methyl propiolate (MP), give a variety of products, all apparently formed by rearrangement of the initial isoxazole 1,3-dipolar cycloadduct, with the type of reaction being dependent on the 2-substituent in 3: the 2-phenyl derivative of 3 gives oxazoloindoles 5, and when 3 posseses a methyl or methylene substituent at C-2, both DMAD and MP give pyrroloindoles 6, with the MP reactions also yielding an azepinoindole 7 in each case.The structures of the products have been established by spectroscopy with those of 5b and 7b being confirmed by X-ray crystallography.
