159184-95-9Relevant academic research and scientific papers
Chromenones derivatives with strong cardiac activating function and pharmaceutical composition containing thereof for preventing or treating heart failure
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Paragraph 0087-0089, (2017/04/13)
Method for preventing or treating composition of the present invention novel compress maul rice field derivatives and including of heart failure, ventricular muscle contraction has excellent effect of increasing myocardial myosin ATPase activation effect, can be useful for the prevention or treatment of heart failure drug. (by machine translation)
3′-Hydroxy-3,4′-dimethoxyflavone blocks tubulin polymerization and is a potent apoptotic inducer in human SK-MEL-1 melanoma cells
Estévez-Sarmiento, Francisco,Said, Mercedes,Brouard, Ignacio,León, Francisco,García, Celina,Quintana, José,Estévez, Francisco
, p. 6060 - 6070 (2017/10/13)
Flavonoids are naturally occurring polyphenolic compounds and are among the most promising anticancer agents. A series of flavonols and their 3-methyl ether derivatives were synthesized and assessed for cytotoxicity. It was found that 3′-hydroxy-3,4′-dime
Exploration of Pharmacophore in Chrysosplenol C as Activator in Ventricular Myocyte Contraction
Venkateswararao, Eeda,Son, Min-Jeong,Sharma, Niti,Manickam, Manoj,Boggu, PullaReddy,Kim, Young Ho,Woo, Sun-Hee,Jung, Sang-Hun
, p. 758 - 763 (2015/07/15)
Chrysosplenol C (4',5,6-trihydroxy-3,3',7-trimethoxyflavone) isolated from Miliusa balansae has unique structural features as a reversible inotropic agent independent of β-adrenergic signaling and with selective activation of cardiac myosin ATPase. Hence, a series of chrysosplenol analogues were synthesized and explored for identification of pharmacophore that is essential for the increasing contractility in rat ventricular myocytes. Analogue 7-chloro-2-(3-hydroxyphenyl)-3-methoxy-4H-chromen-4-one showed highly potent contractility (54.8% at 10 μM) through activating cardiac myosin ATPase (38.7% at 10 μM). Our systematic structure-activity relationship study revealed that flavonoid nucleus of chrososplenol C appears to be an essential basic skeleton and hydrophobic substituent at position 7 of chromenone such as methoxy or chloro enhances the activity. Additionally, our ATPase study suggested that these chrysosplenol analogues have selectivity toward cardiac myosin activation. Thus, the novel flavonone with 3-/7-hydrophobic substituent and 3'-hydrogen bonding donor function is a novel scaffold for discovery of a new positive inotropic agent.
Design, synthesis and biological activity of flavonoid derivatives as selective agonists for neuromedin U 2 receptor
Ma, Ming-Liang,Li, Ming,Gou, Jiao-Jiao,Ruan, Tian-Yu,Jin, Hai-Shan,Zhang, Ling-Hong,Wu, Liang-Chun,Li, Xiao-Yan,Hu, Ying-He,Wen, Ke,Zhao, Zheng
, p. 6117 - 6123 (2015/02/02)
Central neuromedin U 2 receptor (NMU2R) plays important roles in the regulation of food intake and body weight. Identification of NMU2R agonists may lead to the development of pharmaceutical agents to treat obesity. Based on the structure of rutin, a typi
Understanding the cardioprotective effects of flavonols: Discovery of relaxant flavonols without antioxidant activity
Cheng, Xue Qin,Chen, Xingqiang,Hughes, Richard A.,Williams, Spencer J.,Woodman, Owen L.
, p. 1874 - 1884 (2008/12/21)
3′,4′-Dihydroxyflavonol (DiOHF) is a cardioprotective flavonol that can reduce injury after myocardial ischemia and reperfusion and thus is a promising small molecule for the treatment of cardiovascular disease. Like all vasoactive flavonols reported to date, DiOHF is both relaxant and antioxidant, hindering investigation of the relative contribution of each activity for the prevention of reperfusion injury. This study investigates structure-activity relationships of variations at the 3′ and 4′ positions of the B ring of DiOHF and vasorelaxant and antioxidant activities. Relaxation of rat isolated aortic rings precontracted with KCl revealed that the most active flavonols were those with a 4′-hydroxyl group, with the opening of potassium channels as a possible contributing mechanism. For the antioxidant activity, with the exception of DiOHF, none of the flavonols investigated were able to significantly scavenge superoxide radical, and none of the three most potent vasorelaxant flavonols could prevent oxidant-induced endothelial dysfunction. The discovery of single-acting vasorelaxant flavonols without antioxidant activity, in particular 4′-hydroxy-3′-methoxyflavonol, will assist in investigating the mechanism of flavonol-induced cardioprotection.
