53350-27-9Relevant articles and documents
Antischistosomal properties of aurone derivatives against juvenile and adult worms of Schistosoma mansoni
Pereira, Vinicius R.D.,da Silveira, Lígia S.,Mengarda, Ana C.,Alves Júnior, Ismael J.,da Silva, Ohana Oliveira Zuza,Miguel, Fábio Balbino,Silva, Marcos P.,Almeida, Ayla das C.,Torres, Daniel da Silva,Pinto, Priscila de F.,Coimbra, Elaine S.,de Moraes, Josué,Couri, Mara R.C.,da Silva Filho, Ademar A.
, (2020/11/17)
Schistosomiasis is a neglected disease caused by helminth flatworms of the genus Schistosoma, affecting over 240 million people in more than 70 countries. The treatment relies on a single drug, praziquantel, making urgent the discovery of new compounds. A
Development of a novel nitric oxide (NO) production inhibitor with potential therapeutic effect on chronic inflammation
Chen, Lijuan,Fan, Tiantian,Lei, Xiangui,Teichmann, Alexander Tobias,Wang, Amu,Wang, Chao,Wei, Zhe,Wieland, Frank Heinrich,Yang, Youzhe,Yin, Jinxiang,Zhou, Li,Zhu, Yue
supporting information, (2020/03/24)
Inflammation is a complex biological response to stimuli. Activated macrophages induced excessively release of pro-inflammatory cytokines and mediators such as endogenous radical nitric oxide (NO) play a significant role in the progression of multiple inflammatory diseases. Both natural and synthetic chalcones possess a wide range of bioactivities. In this work, thirty-nine chalcones and three related compounds, including several novel ones, based on bioactive kava chalcones were designed, synthesized and their inhibitory effects on NO production in RAW 264.7 cells were evaluated. The novel compound (E)-1-(2′-hydroxy-4′,6′-dimethoxyphenyl)-3-(3-methoxy-4-(3-morpholinopropoxy)phenyl)prop-2-en-1-one (53) exhibited a better inhibitory activity (84.0%) on NO production at 10 μM (IC50 = 6.4 μM) with the lowest cytotoxicity (IC50 > 80 μM) among the tested compounds. Besides, western blot analysis indicated that compound 53 was a potent down-regulator of inducible nitric oxide synthase (iNOS) protein. Docking study revealed that compound 53 also can dock into the active site of iNOS. Furthermore, at the dose of 10 mg/kg/day, compound 53 could both significantly suppress the progression of inflammation on collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) models. In addition, the structure-activity relationship (SAR) of the kava chalcones based analogs was also depicted.
Chalcone analogue and application thereof
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Paragraph 0034-0040; 0085-0086, (2020/07/02)
The invention discloses a chalcone analogue and application thereof, wherein the structure of the chalcone analogue is shown as a formula (I), and R is selected from substituted or unsubstituted arylor heteroaryl; the substituent groups on the aryl group