40554-92-5Relevant academic research and scientific papers
Isorhamnetin biotin probe, synthesis method and application thereof
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Paragraph 0044-0049, (2021/02/10)
The invention relates to an isorhamnetin biotin probe, a synthesis method and application thereof, the probe takes isorhamnetin as a reaction group and biotin as an affinity tag, and has the structureshown as the formula in the specification, wherein X is
Synthesis of 3′-O-Alkyl Homologues and a Biotin Probe of Isorhamnetin and Evaluation of Cytotoxic Efficacy on Cancer Cells
Tursumamat, Nafisa,Yang, Zhuojin,Zheng, Yi,Zhu, Mingyan
, (2021/10/19)
Isorhamnetin is a natural flavonoid which shows a variety of biological activities such as antioxidant, anti-inflammatory and antitumor. In order to identify the cellular binding protein of isorhamnetin as potential anti-cancer target, we first synthesize
Regiospecific synthesis of three quercetin O-β-glucosides of N-acetylglucosamine
Cao, Zhiling,Chen, Jing,Zhu, Dandan,Yang, Zongnan,Teng, Wenqi,Liu, Gaofeng,Liu, Bing,Tao, Chuanzhou
, p. 189 - 193 (2018/05/26)
The regiospecific synthesis of three quercetin O-β-glucosides of N-acetylglucosamine has been achieved in good yield. Selective di- and tri-O-benzylation of quercetin followed by O-glycosylation with 2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-α-d-glucopyranosyl chloride under phase-transfer catalysis conditions yielded, after deacetylation and debenzylation, 3-, 3′- and 4′-glycosylated quercetin.
Quercetin derivative and its preparation method and application
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Paragraph 0037; 0038, (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.
Effects of Functional Groups and Sugar Composition of Quercetin Derivatives on Their Radical Scavenging Properties
Kato, Komei,Ninomiya, Masayuki,Tanaka, Kaori,Koketsu, Mamoru
supporting information, p. 1808 - 1814 (2016/08/02)
Quercetin derivatives are widespread in the plant kingdom and exhibit various biological actions. The aim of this study was to investigate the structure-activity relationships of quercetin derivatives, with a focus on the influence of functional groups and sugar composition on their antioxidant capacity. A series of quercetin derivatives were therefore prepared and assessed for their DPPH radical scavenging properties. Isoquercetin O-gallates were more potent radical scavengers than quercetin. The systematic analysis highlights the importance of the distribution of hydroxy substituents in isoquercetin O-gallates to their potency.
Biological evaluation and SAR analysis of O-methylated analogs of quercetin as inhibitors of cancer cell proliferation
Shi, Zhi-Hao,Li, Nian-Guang,Tang, Yu-Ping,Shi, Qian-Ping,Tang, Hao,Li, Wei,Zhang, Xu,Fu, Hai-An,Duan, Jin-Ao
, p. 455 - 462 (2015/04/14)
Preclinical Research Using a high-throughout screening approach, the anticancer activities of 16 O-methylated (OMe) analogs of quercetin were assessed. The structure-activity relationships showed that OMe moieties at the 4′ and/or 7 positions were important for maintaining inhibitory activities against the 16 cancer cell lines. Furthermore, when the OH groups at the 3′ and 4′ positions were both replaced by OMe moieties, anticancer activity was enhanced.
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
Synthesis and identification of quercetin benzyl ethers
Karimova,Spirikhin,Baltina,Abdullin
, p. 1711 - 1715 (2015/01/09)
We have studied the effects of the benzylating agent character, the reactants ratio, and the solvent nature on the composition of the products of quercetin benzylation. The structure of the products has been confirmed by IR, UV, 1H NMR, 13
Metabolism-based synthesis, biologic evaluation and SARs analysis of O-methylated analogs of quercetin as thrombin inhibitors
Shi, Zhi-Hao,Li, Nian-Guang,Tang, Yu-Ping,Wei-Li,Lian-Yin,Yang, Jian-Ping,Hao-Tang,Duan, Jin-Ao
experimental part, p. 210 - 222 (2012/09/07)
In blood, quercetin is mainly found in metabolized forms. In order to study the activities of these quercetin metabolites in cardiovascular disease, 17 methylquercetin derivatives were synthesized based on metabolism in vivo, their thrombin inhibition activity were evaluated through the analyzation of prothrombin time (PT), activated partial thromboplastin time (APTT), thrombin time (TT) and fibrinogen (FIB). The results showed that 6 methylquercetin derivatives had stronger inhibitory activities than that of quercetin. Preliminary SARs analysis showed that hydroxyl groups at C-3′ and C-4′ position in the B-ring and hydroxyl group at C-3 position in the C-ring played key roles in the thrombin inhibitory activity. The findings of this study would provide information for the exploitation and utilization of quercetin as thrombin inhibitor for thrombotic disease treatment.
Novel quercetin derivatives, their preparation, pharmaceutical compositions containing them and their use
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Page/Page column 8, (2012/07/03)
The invention relates to novel quercetin derivatives and pharmaceutically acceptable salts, hydrates, and solvates and dimers thereof; a process for the preparation of the novel quercetin derivatives and pharmaceutically acceptable salts, hydrates, and so
