862255-02-5Relevant academic research and scientific papers
Synthesis of flavonoids nitrogen mustard derivatives and study on their antitumor activity in vitro
Hao, Haijun,Song, Jinglei,Sun, Hao-Ling,Yan, Xi,Yu, Meixuan
, (2020/02/06)
Several novel flavonoids nitrogen mustard derivatives were synthesized and evaluated for antiproliferative activity against seven human cancer cell lines (HeLa, A549, HepG2, MCF7, SH-SY5Y, PC-3, DU145) by the MTT assay in vitro. The resulting IC50/s
Genistein bridged imidazole derivative synthesis method and use of genistein bridged imidazole derivative in tumor resistance
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Paragraph 0065-0073, (2019/01/20)
The invention provides a genistein derivative shown in the formula (I), wherein R represents a nitrogen-containing heterocyclic group or a substituted nitrogen-containing heterocyclic group, a substituent in the substituted nitrogen-containing heterocycli
Synthesis and biological evaluation of genistein-O-alkylamine derivatives as potential multifunctional anti-Alzheimer agents
Hong, Chen,Guo, Hui-yan,Chen, Shuai,Lv, Jian-wu,Zhang, Xin,Yang, Ya-cheng,Huang, Kang,Zhang, Yi-juan,Tian, Zhi-yong,Luo, Wen,Chen, Yi-ping
, p. 188 - 200 (2018/10/26)
A series of genistein derivatives were synthesized and evaluated as multifunctional anti-Alzheimer agents. The results showed that these derivatives had significant acetylcholinesterase (AChE) inhibitory activity; compound 5a exhibited the strongest inhib
Nitrogen mustard-based flavonoid derivative, preparation method thereof and application in anti-tumor direction
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Paragraph 0066; 0073; 0074, (2019/03/15)
The invention discloses a preparation method of a class of nitrogen mustard-based flavonoid derivatives and application thereof in an anti-tumor activity study. As shown in the formula I and the formula II, n is an integer which is more than or equal to 0
Genistein derivative, as well as preparation method and application thereof
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Paragraph 0053; 0063-0065, (2018/07/07)
The invention provides a genistein derivative, which is as shown in a formula (I), wherein R is alkyl groups of C1 to C5, or aryl groups of C6 to C10, and n is an integer larger than or equal to 1. Compared with the prior art, the genistein derivative pro
Design, synthesis and evaluation of genistein-O-alkylbenzylamines as potential multifunctional agents for the treatment of Alzheimer's disease
Qiang, Xiaoming,Sang, Zhipei,Yuan, Wen,Li, Yan,Liu, Qiang,Bai, Ping,Shi, Yikun,Ang, Wei,Tan, Zhenghuai,Deng, Yong
, p. 314 - 331 (2014/03/21)
A series of genistein derivatives with carbon spacer-linked alkylbenzylamines were designed, synthesized and tested as multifunctional agents for the treatment of Alzheimer's disease (AD). The results showed that most of these compounds exhibited good acetylcholinesterase (AChE) inhibitory activity, with moderate-to-good anti-oxidative activity. Specifically, compounds 10b, 19d and 25d exhibited significant inhibition of β-amyloid (Aβ) aggregation and exhibited metal chelating properties. In particular, 25d inhibited: self-induced Aβ1-42 aggregation, Cu 2+-induced Aβ1-42 aggregation, and human AChE-induced Aβ1-40 aggregation by 35%, 77.8%, and 36.2%, respectively. Moreover, both kinetic analysis of AChE inhibition and the molecular modeling study suggested that 25d binds simultaneously to catalytic active site and peripheral anionic site of AChE. More importantly, compound 25d disassembled the well-structured Aβ fibrils generated by Cu2+-induced Aβ aggregation by 72.1%. Furthermore, the step-down passive avoidance test showed this compound significantly reversed scopolamine-induced memory deficit in mice. These results suggest that 25d may be a promising multifunctional agent for AD treatment.
Synthesis and antimicrobial activities of 7-O-modified genistein derivatives
Zhang, Li-Na,Cao, Ping,Tan, Shu-Hua,Gu, Wen,Shi, Lei,Zhu, Hai-Liang
, p. 1543 - 1551 (2008/09/21)
Three series of genistein derivatives with heterocycles were prepared, in which genistein and heterocyclic moieties were separated by 2-carbon, 3-carbon and 4-carbon spacers. Among the 33 compounds we prepared 11 of them (2c and 5a-j) are reported for the
Genistein derivatives as selective estrogen receptor modulators: Sonochemical synthesis and in vivo anti-osteoporotic action
Wang, Shi F.,Jiang, Qing,Ye, Yong H.,Li, Yang,Tan, Ren X.
, p. 4880 - 4890 (2007/10/03)
Genistein derivatives were synthesized from genistein through a facile sonochemical approach in high yields. The bioassay was performed on ovariectomized (OVX) rats in terms of bone mineral density (BMD) and the weight of bone ash (WBA) to lead to the discovery of eight novel genistein-based selective estrogen receptor modulators. Attention to the structure-activity relationship disclosed that the newly introduced 2-hydroxyethylthio scaffolds were essential for the anti-osteoporotic activity. Moreover, the anti-osteoporotic action of genistein, deprivable by methylation, could be restored and enhanced by subsequent sulfonation. The most promising compound was 4′,5,7-tri[3-(2-hydroxyethylthio)propoxy]isoflavone, displaying 24% (or 8%) increment in BMD and 31% (or 11%) increase in WBA of the femora relative to those discerned with the OVX (or genistein) group. Acute toxicity test showed that none of the active compounds was acutely toxic.
