52273-55-9Relevant academic research and scientific papers
Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models
Romussi, Alessia,Cappa, Anna,Vianello, Paola,Brambillasca, Silvia,Cera, Maria Rosaria,Dal Zuffo, Roberto,Fagà, Giovanni,Fattori, Raimondo,Moretti, Loris,Trifirò, Paolo,Villa, Manuela,Vultaggio, Stefania,Cecatiello, Valentina,Pasqualato, Sebastiano,Dondio, Giulio,So, Chi Wai Eric,Minucci, Saverio,Sartori, Luca,Varasi, Mario,Mercurio, Ciro
supporting information, p. 754 - 759 (2020/03/04)
Lysine-specific demethylase 1 (LSD1 or KDM1A) is a FAD-dependent enzyme that acts as a transcription corepressor or coactivator by regulating the methylation status of histone H3 lysines K4 and K9, respectively. KDM1A represents an attractive target for c
Copper-catalyzed asymmetric silylative cyclization of cyclohexadienone-containing 1,6-enynes
He, Cheng-Yu,Xie, Li-Bo,Ding, Rui,Tian, Ping,Lin, Guo-Qiang
, p. 1682 - 1688 (2019/01/04)
The first copper-catalyzed asymmetric silylative cyclization of cyclohexadienone-containing 1,6-enynes has been accomplished through a tandem process: regioselective silylcupration of terminal unactivated alkynes and subsequently enantioselective conjugate addition to cyclohexadienones. This reaction proceeded smoothly to afford the cis-hydrobenzofuran and cis-hydroindole frameworks bearing two consecutive chiral carbon centers in high to excellent yields and moderate enantioselectivities. Additionally, the cyclization products could be readily subjected to several transformations for elaborating synthetic utilities.
Visible Light-Mediated Conversion of Alcohols to Bromides by a Benzothiadiazole-Containing Organic Photocatalyst
Li, Run,Gehrig, Dominik W.,Ramanan, Charusheela,Blom, Paul W. M.,Kohl, Fabien F.,Wagner, Manfred,Landfester, Katharina,Zhang, Kai A. I.
, p. 3852 - 3859 (2019/07/15)
The search for metal-free, stable and high effective photocatalysts with sufficient photo-redox potentials remains a key challenge for organic chemists. Here, we present a benzothiadiazole-containing molecular organic photocatalyst with redox potentials of ?1.30 V and +1.64 V vs. SCE. The singlet state lifetime is 13 ns. Direct conversion from aliphatic alcohols to bromides has been conducted with the designed organic photocatalyst under visible light irradiation with high efficiency and selectivity. The catalytic efficiency of the novel benzothiadiazole-based photocatalyst is comparable with the state-of-art metal and non-metal catalysts. Furthermore, advanced photophysical studies including time-resolved photoluminescence and transient absorption spectroscopy offer a powerful support for photo-induced electron transfer from photocatalyst to the reactive substrates. Lastly, no photo-bleaching effect is observed, demonstrating the high stability and recyclable of the designed organic photocatalyst. (Figure presented.).
Synthesis and PGE2 inhibitory activity of novel diarylheptanoids
McLane, Richard D.,Le Cozannet-Laidin, Léon,Boyle, Maxwell S.,Lanzillotta, Lindsey,Taylor, Zachary L.,Anthony, Sarah R.,Tranter, Michael,Onorato, Amber J.
, p. 334 - 338 (2018/02/15)
Prostaglandin E2 (PGE2) is a lipid mediator of inflammation and its inhibition has become a popular drug target due to its harmful physiological roles. Diarylheptanoids are one class of compounds that have shown successful inhibition of PGE2. This paper reports the synthesis and PGE2 inhibitory activity of a series of analogues of a naturally occurring diarylheptanoid. The most efficacious compounds were examined for dose-dependent PGE2 inhibition. Among several promising compounds, the lead candidate exhibited an IC50 value of 0.56 ng/μL or 1.7 μM with no detectable toxicity at the highest dose of 10 ng/μL.
Diphenyl sulfate derivatives, preparation method of thereof and fluorophore sensor comprising thereof
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Paragraph 0236-0239, (2017/06/02)
The present invention relates to a diphenyl sulfate derivative, a method for preparing the same, and a fluorescence bio-sensor comprising the same. The diphenyl sulfate derivative having a novel structure according to the present invention traces cells and carries out immuno-fluorescence staining of the mitochondria of the cells satisfactorily. Thus, the diphenyl sulfate sulfate is useful in the glioma-related field and the research field including virus and DNA transfection, and can be used advisably as fluorescence bio-sensor for diagnosing diseases, such as glioma, sarcoma or leukemia.
NITRIC OXIDE DONOR NEPRILYSIN INHIBITORS
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, (2014/01/07)
In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R7, R8, Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
A short and efficient synthesis of a novel diarylheptanoid isolated from pleuranthodium racemigerum
Chang, Ching-Yao
experimental part, p. 286 - 289 (2011/10/13)
The first total synthesis of the linear diarylheptanoid 1-(4"-methoxyphenyl)-7-(4′-hydroxyphenyl)-(E)-hept-2-ene, which has a uniquely nonconjugated olefin, was achieved. The synthetic route employed an olefin cross-metathesis as a key step. Beginning wit
Visible-light-mediated conversion of alcohols to halides
Dai, Chunhui,Narayanam, Jagan M.R.,Stephenson, Corey R.J.
experimental part, p. 140 - 145 (2012/02/06)
The development of new means of activating molecules and bonds for chemical reactions is a fundamental objective for chemists. In this regard, visible-light photoredox catalysis has emerged as a powerful technique for chemoselective activation of chemical bonds under mild reaction conditions. Here, we report a visible-light-mediated photocatalytic alcohol activation, which we use to convert alcohols to the corresponding bromides and iodides in good yields, with exceptional functional group tolerance. In this fundamentally useful reaction, the design and operation of the process is simple, the reaction is highly efficient, and the formation of stoichiometric waste products is minimized.
LTA4H modulators and uses thereof
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Page/Page column 29, (2008/12/07)
Leukotriene A4 hydrolase (LTA4H) inhibitors, compositions containing them, and methods of use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and/or conditions associated with inflammation.
