137109-37-6Relevant articles and documents
The fluorescence properties of 4′-Methoxychalcone derivates modified by substituents and investigation of lysosomal imaging
Cai, Zhengxu,Dong, Yuping,Lin, Na,Shi, Jianbing,Tong, Bin,Wu, Xinghui
, (2022/01/25)
Three types of 4′-methoxychalcone derivatives Cha-1 ~ Cha-9 with different electron-withdrawing or electron-donating substituents at different positions were synthesized and studied. When the A ring has a hydroxyl group at the 2-position, the strong electron-donating groups at the 4-position of the B ring was more conducive to the near-infrared and aggregation-enhanced emission (AEE) features of the compound than the electron withdrawing groups. The single-crystal analysis confirmed that the good planarity of the 4′-methoxychalcone derivatives favors their fluorescence quantum yields. Moreover, chalcone fluorophores with different fluorescence properties could be obtained by modulating substituent at the 2-position of A ring. In addition, Cha-9 was selected as the AEE luminogen to locate the lysosomes in HeLa cells. These results provided fundamental knowledge for the design and application of 4′-methoxychalcone derivatives of aggregation-induced emission (AIE) compounds.
Certain 4-iminoflavones derivatives: Synthesis, docking studies, antiasthmatic and antimicrobial agents
Khah, Shaila,Goyal, Rohit,Chabba, Ankush,Jaiswal, Varun,Sharma, Gaurav,Naushad
, p. 1687 - 1696 (2016/07/06)
In this present study, certain substituted 4-iminoflavone derivatives 5(a-j) were synthesized. All the synthesized compounds were evaluated for antiasthmatic and antimicrobial activity. Among the synthesized compounds, 5f was found to be the most promising against asthmatic models, whilst, 5h was found active against all the microbial strains. Antiasthmatic activity was correlated and evaluated with various models, e.g., citric acid induced cough model, OVA induced asthma model (biochemical estimation for cell infiltrations, estimation of lipid peroxidation and glutathione and estimation of TNF-α and IL-6 and histamine induced response). Compound 5f was found to show 2.20 ± 0.047 number of cough whilst codeine showed 1.40 ± 0.548; compound 5f produced considerable reduction in neutrophils, lymphocytes, eosinophils and leukocytes; decrease in LPO level (lung and BALF) and increment in GSH level (lungand BALF); and decreased the level of TNF-α and IL-6, respectively. On the other hand, 5h showed MIC 6.25 μg/mL against B. subtilis and S. aureus, 3.1 μg/mL against E. coli, 1.55 μg/mL against S. typhi and 6.25 μg/mL against C. albicans, respectively. In addition to gain better understanding on the biological activities of synthesized compounds, molecular docking study was performed within the binding site of human histamine H1 receptor and Glc-6-P synthase revealing compound 5f and 5h as best fit within the respective receptor pockets.
Inhibition of prostaglandin E2 production by synthetic minor prenylated chalcones and flavonoids: Synthesis, biological activity, crystal structure, and in silico evaluation
Rullah, Kamal,Mohd Aluwi, Mohd Fadhlizil Fasihi,Yamin, Bohari M.,Abdul Bahari, Mohd Nazri,Wei, Leong Sze,Ahmad, Syahida,Abas, Faridah,Ismail, Nor Hadiani,Jantan, Ibrahim,Wai, Lam Kok
, p. 3826 - 3834 (2014/09/16)
The discovery of potent inhibitors of prostaglandin E2 (PGE 2) synthesis in recent years has been proven to be an important game changer in pharmaceutical industry. It is known that excessive production of PGE2 triggers a