22479-78-3Relevant academic research and scientific papers
Synthesis and characterization of hyperbranched polyether imides based on 1,3,5-tris[4-(4′-aminophenoxy)phenoxy]benzene
Rigana, M. Fathima,Thirukumaran,Shanthi,Sarojadevi
, p. 33249 - 33258 (2016)
A new triamine monomer 1,3,5-tris[4-(4′-aminophenoxy)phenoxy]benzene, was synthesized by a three step process using hydroquinone, 1-chloro-4-nitrobenzene and 1,3,5-trichlorobenzene. It was successfully polymerized with commercially available dianhydrides [3,3′,4,4′-benzophenonetetracarboxylic dianhydride (BTDA) and pyromellitic dianhydride (PMDA)] into hyperbranched polyimides (HBPIs) by the A2 + B3 method. Different monomer addition methods and different monomer molar ratios resulted in hyperbranched polyimides with amino and anhydride end groups. The structure of the resulting hyperbranched polyimides were characterized by FT-IR, 1H-NMR, 13C-NMR and mass spectral analysis. All synthesized HBPIs were soluble in most common organic solvents. They also exhibit good thermal stability. The Tg of the HBPIs is in the range of 230-260 °C and T10 values are above 450 °C. The dielectric constant of the synthesized HBPIs is in the range of 3.08-3.29 at 1 MHz and dielectric loss is in the range of 0.65-0.82 at 1 MHz.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 00604-00607; 00604, (2021/06/22)
The present invention provides compounds, compositions thereof, and methods of using the same.
In silico molecular docking, synthesis of 4-(4-benzoylaminophenoxy) phenol derivatives as androgen receptor antagonists
Elancheran, Ramakrishnan,Kabilan, Senthamaraikannan,Kotoky, Jibon,Ramanathan, Muthiah,Bhattacharjee, Atanu
, p. 307 - 316 (2019/09/12)
Aim and Objective: To study the structural difference, optimization, molecular docking and development of new benzoyl amino phenoxy phenol derivatives as anti-prostate cancer agents. Materials and Methods: Strategies towards the identification of novel be
Oxidative and Reductive Cross-Coupling Reactions Catalyzed by an Anionic "ligandless" Palladium Complex
Schroeter, Felix,Lerch, Swantje,Strassner, Thomas
supporting information, p. 1614 - 1621 (2019/01/04)
The anionic complex [NBu4][Pd(DMSO)Cl3], which can be synthesized on a gram scale in a single step starting from commercially available starting materials, has been shown to be an active catalyst in the Mizoroki-Heck reaction of aryl halides. We present two new catalytic applications of this complex: the base-free oxidative Heck reaction and the reductive homodimerization of aryl halides. This complex outperformed other palladium salts. In the latter reaction, the catalyst loading could be reduced to 0.01 mol %. The scope of the reactions has been explored, demonstrating the potential of the anionic palladium complex in these catalytic transformations.
Design, synthesis and insecticidal evaluation of aryloxy dihalopropene derivatives
Yang, Ji-Chun,Li, Miao,Wu, Qiao,Liu, Chang-Ling,Chang, Xiu-Hui
, p. 383 - 390 (2016/01/25)
Plutella xylostella (P. xylostella) is a highly migratory, cosmopolitan species and one of the most important pest of cruciferous crops worldwide. Pyridalyl as a novel class of insecticides has good efficacy against P. xylostella. On the basis of the commercial insecticide pyridalyl, a series of new aryloxy dihalopropene derivatives were designed and synthesized by using Intermediate Derivatization Methods. Their chemical structures were confirmed by 1H NMR, high-resolution mass spectrum (HRMS), and single-crystal X-ray diffraction analysis. The insecticidal activities of the new compounds against P. xylostella were evaluated. The results of bioassays indicated that most of the compounds showed moderate to high activities at the tested concentration, especially compounds 10e and 10g displayed more than 75% insecticidal activity against P. xylostella at 6.25 mg/L, while pyridalyl showed 50% insecticidal activity at the same concentration. The field trials result of the insecticidal activities showed that compound 10e as a 10% emulsifiable concentrate (EC) was effective in the control of P. xylostella at 75-150 g a.i./ha, and the mortality of P. xylostella for treatment with compound 10e at 75 g a.i./ha was equivalent to pyridalyl at 105 g a.i./ha.
Synthesis and biological evaluation of XB-1 analogues as novel histamine H3 receptor antagonists and neuroprotective agents
Bao, Xiaofeng,Jin, Yanyan,Liu, Xiaolu,Liao, Hong,Zhang, Luyong,Pang, Tao
, p. 6761 - 6775 (2014/02/14)
A novel class of H3 receptor antagonists, XB-1 analogues based on benzophenone or oxydibenzene scaffolds were synthesized, and their biological activities were evaluated to determine their in vitro neuroprotective effects against Aβ25-35-induced damage in primary cortical neurons and against glutamate-induced neuronal injury in primary cerebellar granule neurons. The results indicated that all of the tested analogues displayed neuroprotective activity at 0.1 μM or 1 μM. These findings may provide new insights into the development of novel promising H3 receptor antagonists with potential neuroprotective activity.
Optimization of 5-hydroxytryptamines as dual function inhibitors targeting phospholipase A2 and leukotriene A4 hydrolase
Meng, Hu,Liu, Ying,Zhai, Yujing,Lai, Luhua
, p. 160 - 167 (2013/03/13)
Dual function inhibitors targeting phospholipase A2 (PLA 2) and leukotriene A4 hydrolase (LTA4H) may balance the arachidonic acid (AA) metabolic network and be used as new anti-inflammatory drugs. In previous study, we discovered multi-target drugs towards the AA metabolic network, among which a dual-target inhibitor (JMC08-4) for human nonpancreatic secretory phospholipase A2 (hnps-PLA 2) and human leukotriene A4 hydrolase (LTA4H-h) was found. Based on the structure of compound JMC08-4, new dual-target inhibitors were designed assisted by molecular docking. In this report, a series of 5-hydroxytryptamine compounds were synthesized; and most of these title compounds showed more potent inhibitory activity than compound JMC08-4 in the in vitro bioassay against these two enzymes. The best one inhibited hnps-PLA 2 and LTA4H-h with IC50 values of 9.2 ± 0.5 μM and 2.4 ± 1.4 μM, respectively.
Design and synthesis of 4-(4-benzoylaminophenoxy)phenol derivatives as androgen receptor antagonists
Yamada, Ayumi,Fujii, Shinya,Mori, Shuichi,Kagechika, Hiroyuki
supporting information, p. 937 - 941 (2013/10/22)
We report the design and synthesis of novel 4-(4-benzoylaminophenoxy)phenol derivatives that bind to the androgen receptor (AR) ligand-binding domain and exhibit potent androgen-antagonistic activity. Compound 22 is one of the most potent of these derivatives, inhibiting the dihydrotestosterone-promoted growth of SC-3 cell line bearing wild-type AR (IC50 0.75 μM), LNCaP cell line bearing T877A-mutated AR (IC50 0.043 μM), and 22Rv1 cell line bearing H874Y-mutated AR (IC50 0.22 μM). Structure-activity relationship studies confirmed that the pharmacophore of these novel AR antagonists is distinct from the nitro- or cyano-substituted anilide substructure of other nonsteroidal AR antagonists. This novel pharmacophore is expected to provide a basis for designing new antiprostate cancer agents.
Design, synthesis and antitumor activity of novel cis-furoquinoline derivatives
Li, Jie,Pei, Shuchen,Zhu, Yingxi,Wu, Jianbo,Chen, Yin,Zhang, Weiyu,Wu, Yong
experimental part, p. 379 - 388 (2012/07/03)
A series of novel cis-furoquinoline derivatives was synthesized and tested for their antitumor activities in vitro against HepG2 cells, Lu-04 cells and Leu02 cells to evaluate structure-activity relationships. Assay-based antiproliferative activity study revealed that several compounds had significant effects on cytotoxicity, among which compounds 2f, 2l, 2q were found to be the most active compounds. Above all, compounds 2f, 2l, 2q would be potential anticancer agents which deserved further research.
Discovery of dual target inhibitors against cyclooxygenases and leukotriene A4 hydrolyase
Chen, Zheng,Wu, Yiran,Liu, Ying,Yang, Suijia,Chen, Yunjie,Lai, Luhua
experimental part, p. 3650 - 3660 (2011/07/08)
Dual target inhibitors against COX-2 and LTA4H were designed by adding functional groups from a marketed COX-2 inhibitor, Nimesulide, to an existing LTA4H inhibitor 1-(2-(4-phenoxyphenoxy) ethyl) pyrrolidine. A series of phenoxyphenyl pyrrolidine compounds were synthesized and tested for their inhibition activities using enzyme assays and human whole blood assay. Introduction of small electron withdrawing groups like NO2 and CF3 in the ortho-position of the terminal phenyl ring was found to change the original single target LTA4H inhibitor to dual target LTA4H and COX-2 inhibitors. Compound 5a and 5m showed dual LTA 4H and COX-2 inhibition activities in the enzyme assays and the HWB assay with IC50 values in the micromolar to submicromolar range. As their activities in HWB assay were comparable to the two starting single target inhibitors, the two compounds are promising for further studies. The strategy used in the current study may be generally applicable to other dual target drug designs.
