862255-00-3Relevant 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)
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
Nitrogen mustard-based flavonoid derivative, preparation method thereof and application in anti-tumor direction
-
Paragraph 0065; 0066, (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
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
Genistein derivative, as well as preparation method and application thereof
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Paragraph 0053; 0055-0057, (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
Composition of multiple isoflavone derivatives, preparing method and medical application
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Paragraph 0042; 0043; 0044-0047; 0068; 0083-0088; 0104-0110, (2017/02/24)
The invention discloses a composition of multiple isoflavone derivatives, and further discloses a preparing method of the composition and medical application of the composition in treating diabetes. The composition of the isoflavone derivatives is prepare
Design, synthesis, and evaluation of novel fluoroquinolone-flavonoid hybrids as potent antibiotics against drug-resistant microorganisms
Xiao, Zhu-Ping,Wang, Xu-Dong,Wang, Peng-Fei,Zhou, Yin,Zhang, Jing-Wen,Zhang, Lei,Zhou, Jiao,Zhou, Sha-Sha,Hui, Ouyang,Lin, Xiao-Yi,Mustapa, Manzira,Reyinbaike, Asaimuguli,Zhu, Hai-Liang
, p. 92 - 100 (2014/05/06)
Based on a rationally conceived pharmacophore model to build a multi-target bacterial topoisomerase inhibitor, twenty-one fluoroquinolone-flavonoid hybrids were synthesized. Some obtained hybrids show excellent antibacterial activity against drug-resistant microorganisms with narigenin-ciprofloxacin being the most active, showing 8, 43, 23 and 88 times better activity than ciprofloxacin against Escherichia coli ATCC 35218, Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 25923 and Candida albicans ATCC 90873, respectively. Drug accumulation and DNA supercoiling assays of two active analogues revealed potent inhibition of both the DNA gyrase and efflux pump, confirming the desired dual mode of action. Molecular docking study disclosed that the introduced flavonoid moiety not only provides several additional interactions but also does not disturb the binding mode of the floxacin moiety. Our data also demonstrated that development of antifungals is possible from fluoroquinolones modified at C-7 position.
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.
