Match!

Fluorine-Containing Chrysin Derivatives: Synthesis and Biological Activity

Published on Sep 26, 2019in Natural Product Communications0.554
· DOI :10.1177/1934578X19878921
Yue Zhu (University of South China), Xu Yao (University of South China)+ 4 AuthorsXing Zheng9
Estimated H-index: 9
(University of South China)
Abstract
Chrysin, a flavonoid, has played a great role in the fields of anticancer, antibacterial, and antiviral drug discovery. A large number of chrysin derivatives have been synthesized recently. The flu...
  • References (54)
  • Citations (0)
📖 Papers frequently viewed together
14 Citations
4 Citations
78% of Scinapse members use related papers. After signing in, all features are FREE.
References54
Newest
#1Shen-Zhen Ren (NU: Nanjing University)H-Index: 5
#2Zhong-Chang Wang (NU: Nanjing University)H-Index: 11
Last. Hai-Liang Zhu (NU: Nanjing University)H-Index: 38
view all 10 authors...
Abstract The overexpress of COX-2 was clearly associated with carcinogenesis and COX-2 as a possible target has long been exploited for cancer therapy. In this work, we described the design and synthesis of a series of diarylpyrazole derivatives integrating with chrysin. Among them, compound e9 exhibited the most potent inhibitory activity against COX-2 and antiproliferative activity against Hela cells with IC 50 value of 1.12 μM. Further investigation revealed that e9 could induce apoptosis of ...
6 CitationsSource
#1Kazuhiro J. Fujimoto (Hokuriku University)H-Index: 2
#2Daiki Nema (Hokuriku University)H-Index: 1
Last. Tsugiya Murayama (Hokuriku University)H-Index: 18
view all 8 authors...
Abstract A novel type of antiviral agent for human cytomegalovirus (HCMV) is required, because the appearance of ganciclovir (GCV) resistant viruses has been reported. Tricin (4′,5,7-trihydroxy-3′,5′-dimethoxyflavone) has been shown to suppress significantly HCMV replication in human embryonic lung (HEL) fibroblast cells. Recently, we revealed that the action of tricin is different from that of GCV and cyclin-dependent kinase 9 (CDK9) is one of the target proteins of tricin. These results sugges...
2 CitationsSource
#1Renuka Mani (Annamalai University)H-Index: 3
#2Vijayakumar Natesan (Annamalai University)H-Index: 3
Abstract In recent years, public and scientific interest in plant flavonoids has tremendously increased because of their postulated health benefits. This review was mainly focuses on the flavone chrysin (5,7-dihydroxyflavone), which occurs naturally in many plants, honey, and propolis. A number of in vitro and in vivo studies have revealed the therapeutic effects of chrysin against various diseases. In general, chrysin exhibits many biological activities and pharmacological effects, including an...
23 CitationsSource
#1Rajpratap Kshatriya (Institute of Chemical Technology)H-Index: 2
#2Valmik P. Jejurkar (Institute of Chemical Technology)H-Index: 2
Last. Satyajit Saha (Institute of Chemical Technology)H-Index: 7
view all 3 authors...
Abstract Flavones are present in a variety of medicines and natural products and are important structural motif due to their unique mode of physiological action. Hence the structural importance of flavone moiety has elicited a great deal of interest in the field of organic synthesis and chemical biology to develop some new and improved synthesis of this molecular skeleton. Herein, we have described an up to date overview on the recent advances in the diverse synthetic methodologies of flavones. ...
7 CitationsSource
#1Jubo Wang (CPU: China Pharmaceutical University)H-Index: 1
#2Raoling Ge (CPU: China Pharmaceutical University)H-Index: 4
Last. Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 10
view all 7 authors...
Abstract Phenotypic screening of high quality compound library is one of the most effective strategy to obtain novel bioactive compounds. Recently, our group have constructed a Wogonin-scaffold library with substituents diversity and successfully obtained a series of potent compounds. Herein, we reported the synthesis of these compounds and evaluated the in vitro antitumor activity against a panel of human tumor cell lines. Most of them showed good activity with a broad spectrum and preliminary ...
3 CitationsSource
#1Sergio F. Fonseca (UFPEL: Universidade Federal de Pelotas)H-Index: 2
#2Nathalia B. Padilha (UFPEL: Universidade Federal de Pelotas)H-Index: 3
Last. Eder J. Lenardão (UFPEL: Universidade Federal de Pelotas)H-Index: 29
view all 12 authors...
Abstract Herein we report the use of ultrasonic irradiation (US) in the synthesis of six new semi-synthetic selenium-containing chrysin derivatives by a simple and effective methodology utilizing CuI as catalyst, in good to excellent yields (60–89%). It was observed that US accelerates the reaction compared to conventional heating with excellent selectivity for diselenylated products. Compounds were tested for their antioxidant and anticancer activities in vitro and it was observed that the pres...
16 CitationsSource
#1Xinli Li (Yantai University)H-Index: 1
#2Yi Cai (Yantai University)H-Index: 2
Last. Qing-Guo Meng (Yantai University)H-Index: 3
view all 4 authors...
In order to search for drugs with excellent antibacterial activities, a series of novel chrysin derivatives were designed, synthesized, and evaluated as antibacterial agents. Results of the preliminary antibacterial tests against six human pathogenic bacteria in vitro showed that these compounds exhibited activities to some extent, and some displayed excellent activities than the natural parent chrysin, while some were even more potent than the positive drug Penicillin. Moreover, the molecular m...
3 CitationsSource
#1Majid Zeinali (MUMS: Mashhad University of Medical Sciences)H-Index: 3
Last. Hossein Hosseinzadeh (MUMS: Mashhad University of Medical Sciences)H-Index: 49
view all 3 authors...
Abstract Inflammation and the pro-inflammatory cytokines are associated with numerous chronic diseases. Studies suggest that flavonoids, plant polyphenolic compound derivatives from natural origin, have a wide range of putative biological activities. Similar to other flavonoids, chrysin (CH) by its anti-oxidative and anti-inflammatory effects is a potential prophylactic agent in immunopathological and physicochemical injuries. This is an overview on putative immunomodulatory activities of flavon...
32 CitationsSource
#1Suyun Lin (NCU: Nanchang University)H-Index: 5
#2Li Zeng (NCU: Nanchang University)H-Index: 5
Last. Deming Gong (University of Auckland)H-Index: 10
view all 5 authors...
Abstract Xanthine oxidase (XO) is a key enzyme catalyzing hypoxanthine to xanthine and then uric acid causing hyperuricemia. A Cu(II) complex of chrysin was synthesized and characterized by UV–vis absorption, Fourier transform infrared, nuclear magnetic resonance ( 1 H NMR) and mass spectroscopy studies. The interaction of Cu(II)-complex with XO was investigated by spectroscopic methods and molecular simulation. The Cu(II)-chrysin complex exhibited a better inhibitory ability (IC 50 = 0.82 ± 0.0...
5 CitationsSource
#1Jinlei Bian (CPU: China Pharmaceutical University)H-Index: 10
#2Tinghan Li (CPU: China Pharmaceutical University)H-Index: 3
Last. Zhiyu Li (CPU: China Pharmaceutical University)H-Index: 22
view all 6 authors...
Abstract A novel series of 49 wogonin derivatives were synthesized by introducing group at 7-, 8- or B ring of wogonin. The cytotoxic activities against HepG2, A549 and BCG-823 cancer cell lines were also investigated in vitro . Several of them showed obvious cytotoxic activities and compound 3h possessed the highest potency against HepG2, A549, and BCG-823 with IC 50 values of 1.07 μM, 1.74 μM and 0.98 μM, respectively. A quantitative structure-activity relationship (QSAR) study of these synthe...
5 CitationsSource
Cited By0
Newest