143631-95-2Relevant academic research and scientific papers
POLYPHENOL-PEPTIDE CONJUGATES FOR NUCLEAR-TARGETED DELIVERY
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, (2020/07/15)
The present invention relates to a polyphenol-peptide conjugate composed of: (i) a peptide comprising the amino acid sequence Arg-Arg-X1-Leu, wherein X1 refers to one or two hydrophobic amino acids selected independently from lie, Leu, Val, Phe, Trp, and
Design, synthesis and pharmacological evaluation of ester-based quercetin derivatives as selective vascular KCa1.1 channel stimulators
Carullo, Gabriele,Ahmed, Amer,Trezza, Alfonso,Spiga, Ottavia,Brizzi, Antonella,Saponara, Simona,Fusi, Fabio,Aiello, Francesca
, (2020/11/04)
Quercetin represents one of the most studied dietary flavonoids; it exerts a panel of pharmacological activities particularly on the cardiovascular system. Stimulation of vascular KCa1.1 channels contributes to its vasorelaxant activity, which
Preparation method of 3,5,3',4'-tetraacetoxy-7-hydroxyflavone
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Paragraph 0026-0039, (2020/07/02)
The invention provides a preparation method of 3,5,3',4'-tetraacetoxy-7-hydroxyflavone. The method comprises the following steps: in the presence of a solvent, mixing 3,5,7,3',4'-pentaacetoxyflavone,pyridine hydrochloride and silica gel; and then, after the solvent is removed, carrying out a reaction at a first temperature to obtain the 3,5,3',4'-tetraacetoxy-7-hydroxyflavone. According to the preparation method disclosed by the invention, the position 7 of 3,5,7,3',4'-pentaacetoxyflavone is subjected to a deacetylation reaction in a high-selectivity manner by virtue of the synergistic effectof the silica gel and pyridine hydrochloride, and reagents with relatively high toxicity are not used, so the preparation method is high in safety and simple to operate.
Silica particles with a quercetin-R5 peptide conjugate are taken up into HT-29 cells and translocate into the nucleus
Del Favero, Giorgia,Bialas, Friedrich,Grabher, Stephanie,Wittig, Anja,Br?uer, Birgit,Gerthsen, Dagmar,Echalier, Cécile,Kamalov, Meder,Marko, Doris,Becker, Christian F. W.
, p. 9649 - 9652 (2019/08/15)
Intracellular delivery of bioactive polyphenols is currently evaluated as a protective strategy for cells under pharmaceutical stress. To this end, the 20mer R5 peptide from the marine diatom C. fusiformis was N-terminally modified with a quercetin deriva
Quercetin derivative and its preparation method and application
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, (2018/01/19)
The invention discloses a quercetin derivative and a preparation method and application thereof. The preparation method comprises the following steps: firstly using dichlorodiphenylmethane to protect quercetin o-diphenol hydroxyl, combining a benzyl protection group to obtain the selectively protected quercetin derivative, and then independently reacting with dimethyl sulfate, diethyl sulfate, allyl bromide, paratoluensulfonyl chloride and acetic anhydride respectively to generate corresponding quercetin derivatives. All of the prepared derivative compounds have NRK-49F proliferation activity inhibition superior to that of quercetin. The quercetin derivatives 20a-1, 14a-1 and 23d-1 compositely replaced by methyl and p-tosyl have higher inhibition NRK-49F proliferation activity, and the inhibition ratio respectively reaches 86.33%, 78.04% and 75.91%. Thus, the currently obtained quercetin derivative compounds have obvious inhibition effect on kidney fibroblast NRK-49F proliferation.
Method for preparing 3,3',4',5-tetra-O-acylated quercetin
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Paragraph 0018; 0019, (2016/11/24)
The invention relates to the field of organic small molecule synthesis, in particular to a technology for synthesizing 3,3',4',5-tetra-O-acylated quercetin. The technology comprises the synthesizing steps that 1, quercetin serves as a substrate, acyl chlo
Utilization of the inherent nucleophile for regioselective O-acylation of polyphenols via an intermolecular cooperative transesterification
Liu, Jingchao,Fu, Junjie,Li, Wenlong,Zou, Yu,Huang, Zhangjian,Xu, Jinyi,Peng, Sixun,Zhang, Yihua
supporting information, p. 4103 - 4110 (2016/07/06)
A green and efficient method for regioselective O-acylation of polyphenols has been developed. The acylation can be carried out in potassium carbonate/dimethyl sulphoxide system by utilizing the ‘inherent nucleophile’ via an intermolecular cooperative transesterification under mild condition. This method shows particular advantage in regioselective acylation of polyphenols bearing 2′,4′-dihydroxyacetophenone moiety and can be extended to the synthesis of mono or multiple acetates of polyphenols without this moiety in good yields. Compared with other reported approaches, this method is endowed with atom economy and is more environment-friendly for avoiding the use of any metal-based catalysts.
Discovery of metal ions chelator quercetin derivatives with potent anti-HCV activities
Zhong, Dongwei,Liu, Mingming,Cao, Yang,Zhu, Yelin,Bian, Shihui,Zhou, Jiayi,Wu, Fengjie,Ryu, Kum-Chol,Zhou, Lu,Ye, Deyong
, p. 6978 - 6999 (2015/05/13)
Analogues or isosteres of α,γ-diketoacid (DKA) 1a show potent inhibition of hepatitis C virus (HCV) NS5B polymerase through chelation of the two magnesium ions at the active site. The anti-HCV activity of the flavonoid quercetin ( 2) could partly be attri
Design and discovery of flavonoid-based HIV-1 integrase inhibitors targeting both the active site and the interaction with LEDGF/p75
Li, Bo-Wen,Zhang, Feng-Hua,Serrao, Erik,Chen, Huan,Sanchez, Tino W.,Yang, Liu-Meng,Neamati, Nouri,Zheng, Yong-Tang,Wang, Hui,Long, Ya-Qiu
, p. 3146 - 3158 (2014/06/09)
HIV integrase (IN) is an essential enzyme for the viral replication. Currently, three IN inhibitors have been approved for treating HIV-1 infection. All three drugs selectively inhibit the strand transfer reaction by chelating a divalent metal ion in the
Quercetin-POC conjugates: Differential stability and bioactivity profiles between breast cancer (MCF-7) and colorectal carcinoma (HCT116) cell lines
Cho, Suh Young,Kim, Mi Kyoung,Park, Kwang-Su,Choo, Hyunah,Chong, Youhoon
, p. 1671 - 1679 (2013/05/08)
In the course of our ongoing efforts to develop novel quercetin conjugates with enhanced stability profiles, we introduced an isopropyloxycarbonylmethoxy (POC) group to 7-OH and/or 3-OH of quercetin and prepared three novel quercetin conjugates. The querc
