93876-57-4Relevant academic research and scientific papers
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
Chromenones derivatives with strong cardiac activating function and pharmaceutical composition containing thereof for preventing or treating heart failure
-
Paragraph 0081-0083; 0085, (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)
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.
