58528-03-3Relevant articles and documents
Synthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety
Han, Xu,Liu, Xin Hua,Ma, Duo,Yu, Yun Long,Zhang, Zhao Yan
, p. 344 - 360 (2021/01/06)
Based on previous studies, 66 2-phenyl-4H-chromone derivatives containing amide and 1,3,4-oxadiazole moieties were prepared as potential telomerase inhibitors. The results showed most of the title compounds exhibited significantly inhibitory activity on telomerase. Among them, some compounds demonstrated the most potent telomerase inhibitory activity (IC50 50 = 6.41 μM). In addition, clear structure–activity relationships were summarised, indicating that the substitution of the methoxy group and the position, type and number of the substituents on the phenyl ring had significant effects on telomerase activity. Among them, compound A33 showed considerable inhibition against telomerase. Flow cytometric analysis showed that compound A33 could arrest MGC-803 cell cycle at G2/M phase and induce apoptosis in a concentration-dependent way. Meanwhile, Western blotting revealed that this compound could reduce the expression of dyskerin, which is a fragment of telomerase.
Flavonoid aromatizing enzyme inhibitor as well as preparation method and application thereof
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Paragraph 0039, (2018/07/30)
The invention relates to a flavonoid aromatizing enzyme inhibitor. Through cyanomethylation reaction and alkylation reaction, some substituted groups on the mother ring of a flavonoid compound are changed and a series of flavonoid compounds and derivatives thereof are synthesized. The structural general formula can be shown in the general formula in claims. In the structural general formula, R1 isselected from any one of -OH or -H, R2 is selected from any one of -H, -OCH3 or -OH, R3 is selected from any one of -H, -OH, -OCH2CN or -OCH3, R4 is selected from any one of -H, -OH, -CH2Ph or -2-(2-methoxy-2-oxo ethyl)benzyloxy, R5 is selected from any one of -H, -OCH2Ph or -OCH3, and R6 is selected from any one of -H, -OH or -OCH3. The flavonoid compounds have good inhibition effect on aromatizing enzyme; through activity test, the maximal value IC50 of inhibiting the activity of the aromatizing enzyme by the inhibitor is equal to 0.251 [mu]mol/L.
Design, synthesis, and antiviral activity of novel rutin derivatives containing 1, 4-pentadien-3-one moiety
Han, Yu,Ding, Yan,Xie, Dandan,Hu, Deyu,Li, Pei,Li, Xiangyang,Xue, Wei,Jin, Linhong,Song, Baoan
, p. 732 - 737 (2015/02/05)
Rutin (compound 5) and some compounds (compounds 1e4 and 6) were isolated from Artemisia princeps Pamp (A. princeps Pamp.) and a series of novel rutin derivatives containing 1,4-pentadien-3-one moiety were designed and synthesized. The target compounds were characterized by proton nuclear magnetic resonance spectroscopy (1H NMR), carbon nuclear magnetic resonance spectroscopy (13C NMR), and ESIMS. Bioassay results indicated that some of the compounds showed good to excellent antiviral activities against tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV) at 500 μg/mL in vivo. The 50% effective concentrations (EC50) of the compound 7r against CMV was 394.78 μg/mL, which was better than that of Ningnanmycin (432.22 μg/mL). These results indicated that novel rutin derivatives containing 1,4-pentadien-3-one moiety can effectively control CMV.