51251-55-9Relevant academic research and scientific papers
Anti-tumor compound NY and series of derivatives thereof
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Paragraph 0058-0059; 0062-0063; 0068-0069, (2020/05/02)
The invention relates to an anti-tumor compound NY and a series of derivatives thereof, and an application of the anti-tumor compound NY and the series of derivatives of the anti-tumor compound NY inmedicines. According to the invention, ADAM17 is used as a target spot to design and completely synthesize 15 compounds of NY series; and the antitumor activity of the 15 compounds of the NY series isverified; thus, a potential antitumor activity drug is provided clinically.
Magnetic Nanoparticle Anchored Deep Eutectic Solvents as a Catalyst for the Etherification and Amination of Naphthols
Zamani, Parisa,Ozdemir, John,Ha, Yumi,Benamara, Mourad,Kuchuk, Adrian V.,Wang, Tengjiao,Chen, Jingyi,Khosropour, Ahmad R.,Beyzavi, M. Hassan
supporting information, p. 4372 - 4380 (2018/10/15)
Herein, we introduce a reusable catalyst consisting of a deep eutectic solvent made up of choline chloride and p-toluene sulfonic acid (pTSA) covalently immobilized on magnetic nanoparticles (MNPs) as an agent for chemoselective direct ipso etherification and amination of naphthols. The bonding of the DES to the surface of the nanoparticles has increased the catalytic activity of the DES and also has simplified catalyst recovery from the reaction mixture. The MNP bound DES particles with an average size of 12±2 nm was characterized by FTIR, PXRD, HRTM, TGA, and VSM. For 16 tested etherification reactions, the functionalized magnetite nanoparticle catalyst gave an average yield of 84%; for 5 tested aminations the average yield was 77%. For all 23 tested reactions the yield was above 70% and pTSA Br?nsted acid loading was only 0.45 mol%. The catalytic performance could be attributed to the dispersion of the nanoparticles, strong DES-support interactions and interactions of the hydrogen donor species with naphthols. This work is the first catalytic examination of PDES covalently bonded on MNPs as a platform for organic transformations. (Figure presented.).
Methods of Treating Hepatitis C Virus with Oxoacetamide Compounds
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, (2011/06/10)
Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.
Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines
Mewshaw, Richard E.,Zhou, Dahui,Zhou, Ping,Shi, Xiaojie,Hornby, Geoffrey,Spangler, Taylor,Scerni, Rosemary,Smith, Deborah,Schechter, Lee E.,Andree, Terrance H.
, p. 3823 - 3842 (2007/10/03)
N-Aryloxylethylindolealkylamines (5) having dual 5-HT transporter and 5-HT1A affinity are described. These compounds represent truncated analogues of our previously reported piperidinyl derivatives (3). Compounds in this investigation were found to have more similar affinities and functional activities for the 5-HT1A receptor and 5-HT transporter. Though 5-HT1A antagonism is not consistently observed throughout series 5, several molecular features were found to be essential to obtain high and balanced activities. The proper placement of a heteroatom in the aryl ring and the length of the linkage used to tether the indole moiety had significant influence on 5-HT1A and 5-HT transporter affinities. Introduction of a halogen into the aryl ring usually lowered intrinsic activity and in some cases led to full 5-HT1A antagonists. Compounds 33 and 34 were observed to be full 5-HT1A antagonists with Ki values of approximately 30 nM for the 5-HT1A receptor and Ki values of 5 and 0.5 nM for the 5-HT transporter, respectively. Unfortunately, similar to our previous series (3), compounds in this report also had high affinity for the α1 receptor.
