65819-34-3Relevant academic research and scientific papers
Iron-Catalyzed Nitrene Transfer Reaction of 4-Hydroxystilbenes with Aryl Azides: Synthesis of Imines via C=C Bond Cleavage
Peng, Yi,Fan, Yan-Hui,Li, Si-Yuan,Li, Bin,Xue, Jing,Deng, Qing-Hai
supporting information, p. 8389 - 8394 (2019/10/16)
C=C bond breaking to access the C=N bond remains an underdeveloped area. A new protocol for C=C bond cleavage of alkenes under nonoxidative conditions to produce imines via an iron-catalyzed nitrene transfer reaction of 4-hydroxystilbenes with aryl azides is reported. The success of various sequential one-pot reactions reveals that the good compatibility of this method makes it very attractive for synthetic applications. On the basis of experimental observations, a plausible reaction mechanism is also proposed.
Synthesis and cytotoxic effects on pancreatic cancer cells of resveratrol analogs
De Filippis, Barbara,De Lellis, Laura,Florio, Rosalba,Ammazzalorso, Alessandra,Amoia, Pasquale,Fantacuzzi, Marialuigia,Giampietro, Letizia,Maccallini, Cristina,Amoroso, Rosa,Veschi, Serena,Cama, Alessandro
, p. 984 - 991 (2019/05/10)
In this study, a series of resveratrol analogs was synthesized and the effects on the viability of pancreatic cancer cell lines were evaluated. The new molecules were designed by removing the 3- and 5-OH groups of resveratrol, and by incorporating other s
Chemo-enzymatic synthesis of (: E)-2,3-diaryl-5-styryl- trans -2,3-dihydrobenzofuran-based scaffolds and their in vitro and in silico evaluation as a novel sub-family of potential allosteric modulators of the 90 kDa heat shock protein (Hsp90)
Bassanini, Ivan,D'Annessa, Ilda,Costa, Massimo,Monti, Daniela,Colombo, Giorgio,Riva, Sergio
, p. 3741 - 3753 (2018/05/31)
Herein we propose a facile, versatile and selective chemo-enzymatic synthesis of substituted (E)-2,3-diaryl-5-styryl-trans-2,3-dihydrobenzofurans based on the exploitation of the laccase-mediated oxidative (homo)coupling of (E)-4-styrylphenols. Thanks to this novel synthetic strategy, a library of benzofuran-based potential allosteric activators of the Heat shock protein 90 (Hsp90) was easily prepared. Moreover, considering their structural analogies to previously reported allosteric modulators, the sixteen new compounds synthesized in this work were tested in vitro for their potential stimulatory action on the ATPase activity of the molecular chaperone Hsp90. Combining experimental and computational results, we propose a mechanism of action for these compounds, and expand the structure-activity relationship (SAR) information available for benzofuran-based Hsp90 activators.
Decarboxylation of α,β-unsaturated aromatic lactones: Synthesis of: E-ortho -hydroxystilbenes from 3-arylcoumarins or isoaurones
Huang, Xihua,Liu, Jie,Sheng, Jianfei,Song, Xianheng,Du, Zhibo,Li, Mingkang,Zhang, Xuejing,Zou, Yong
, p. 804 - 808 (2018/03/06)
A simple and environmentally friendly strategy for the synthesis of E-ortho-hydroxystilbenes has been established. Two kinds of α,β-unsaturated aromatic lactones, i.e. the 3-arylcoumarins and the isoaurones, could both readily undergo a cascade hydrolyzation/decarboxylation reaction in the presence of KOH in ethylene glycol to afford the desired E-ortho-hydroxystilbenes in moderate to high yields.
SQUALENE COMPOUNDS AS MODULATORS OF LDL-RECEPTOR EXPRESSION
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Paragraph 0004; 0013, (2016/04/20)
The present invention relates to compounds that modify low density lipoprotein receptor (LDLR) expression. The compounds have the structural formula I shown below: wherein m, R1, n, R2 and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with elevated levels of low density lipoprotein cholesterol (LDL-C).
PPARα agonists based on stilbene and its bioisosteres: Biological evaluation and docking studies
De Filippis, Barbara,Agamennone, Mariangela,Ammazzalorso, Alessandra,Bruno, Isabella,D'Angelo, Alessandra,Di Matteo, Mauro,Fantacuzzi, Marialuigia,Giampietro, Letizia,Giancristofaro, Antonella,MacCallini, Cristina,Amoroso, Rosa
supporting information, p. 1513 - 1517 (2015/08/18)
A new series of gemfibrozil analogues conjugated with trans-stilbene were synthesized and evaluated with the aim of developing new PPARα agonists. The phenyls of stilbene were modified by introducing substituents in the ortho or para position and only the
Polystyrene resin supported palladium(0) (Pd@PR) nanocomposite catalyzed synthesis of β-aryl and β,β-diaryl unsaturated scaffolds following tandem approaches
Shil, Arun K.,Das, Pralay
, p. 24859 - 24863 (2015/03/30)
A one pot general tandem procedure is described for β-aryl and β,β-diaryl alkenes synthesis following an alternative to the classical approaches by using aryl aldehyde as one of the starting materials. The developed polystyrene resin supported palladium(0) (Pd@PR) nanocomposite has been applied in an unprecedented sequential condensation-decarboxylation-Heck (CDH) and condensation-Heck (CH) strategies to generate the substituted alkenes (C6(C6)CC-C, C6-CC-C6, and C6(C6)CC-CO-C6 units) under ligand, and additive free milder basic reaction conditions. The added momentous benefit over the classical methodologies is in terms of its multi-component approach to achieve the desired products without tedious step wise purifications. This journal is
Inhibitory effect of cytotoxic stilbenes related to resveratrol on the expression of the VEGF, hTERT and c-Myc genes
Martí-Centelles, Rosa,Falomir, Eva,Murga, Juan,Carda, Miguel,Marco, J. Alberto
supporting information, p. 488 - 496 (2015/10/05)
A group of thirty-nine stilbene derivatives, prepared by means of Heck coupling reactions, has been investigated for their cytotoxicity, as well as for their ability to inhibit the production of the vascular endothelial growth factor (VEGF) and the activation of telomerase. The ability of these compounds to inhibit proliferation of two tumoral cell lines (HT-29 and MCF-7) and one non tumoral cell line (HEK-293) was first determined. Subsequently, we determined the capacity of the compounds to inhibit the secretion of VEGF in the aforementioned cell lines and to downregulate the expression of the VEGF, hTERT and c-Myc genes, the two latter involved in the control of the activation of telomerase. One of the synthetic stilbenes, (E)-4-(4-methoxystyryl)aniline, showed strong cytotoxicity and proved able to cause a marked decrease both in the secretion of VEGF and in the expression of the hTERT and c-Myc genes, in all cases at concentrations in the low nanomolar range.
Transition-metal-free semihydrogenation of diarylalkynes: Highly stereoselective synthesis of trans -alkenes using Na2S·9H 2O
Chen, Zhengwang,Luo, Miaoting,Wen, Yuelu,Luo, Guotian,Liu, Liangxian
supporting information, p. 3020 - 3023 (2014/06/23)
A highly stereoselective and efficient transition-metal-free semihydrogenation of internal alkynes to E-alkenes using cheap and green water as hydrogen donor is described. The reactions are conducted under convenient conditions and provide products in good to excellent yields, with broad substrate scope, including a variety of diarylalkynes.
Aerobic oxidative coupling of resveratrol and its analogues by visible light using mesoporous graphitic carbon nitride (mpg-C3N4) as a bioinspired catalyst
Song, Tao,Zhou, Bo,Peng, Guang-Wei,Zhang, Qing-Bao,Wu, Li-Zhu,Liu, Qiang,Wang, Yong
supporting information, p. 678 - 682 (2014/01/23)
The first aerobic oxidative coupling of resveratrol and its analogues by mesoporous graphitic carbon nitride as a bioinspired catalyst with visible light has been developed. With this method, δ-viniferin and its analogues were synthesized in moderate to high yield. The metal-free conditions, visible-light irradiation, and the ideal oxidant, molecular oxygen, make this coupling reaction environmental friendly and practical. Copyright
