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아라자나쉬레스타,Aastha Shrestha,박필훈,이응석 대한화학회 2019 Bulletin of the Korean Chemical Society Vol.40 No.7
Oxidative stress due to overproduction of reactive oxygen species (ROS) plays a major role in inflammation, cancer, and neurodegenerative disorders. In this study, 60 chalcone derivatives with fluorine (F), trifluoromethyl (CF3), trifluoromethoxy (OCF3), chlorine (Cl), and bromine (Br) in ring A and with or without hydroxy (OH) in ring B were designed, synthesized, and screened for inhibitory activity against lipopolysaccharide (LPS)-stimulated ROS production in RAW 264.7 macrophages. Structure?activity relationship study revealed the importance of a hydroxyl moiety in ring B for enhancing inhibitory activity of ROS production. Furthermore, a hydroxyl group at the ortho-position is more essential for inhibition of ROS production followed by meta- and para-positions. Among all, compound 27 that contains para-chlorine moiety in ring A and ortho-hydroxy in ring B displayed the strongest inhibitory activity (IC50 = 3.42??M) against LPS-stimulated ROS production in RAW264.7 macrophages.
Pramila Katila,Aastha Shrestha,아라자나쉬레스타,Ritina Shrestha,박필훈,이응석 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.12
A new series of thirty-two fluorinated and/or hydroxylated 2-arylidene-1-indanone derivatives were systematically designed, synthesized, and evaluated for their inhibitory activity against LPS-stimulated ROS production in RAW 264.7 macrophages. 5/6-Fluoro-1-indanone or 4-, 5-, 6-, or 7-hydroxyindanone moiety along with ortho-, meta-, or para-hydroxyphenyl, furanyl or thiophenyl moiety was prepared and evaluated. Among the synthesized compounds, compound 11 possessing 6-hydroxy-1-indanone moiety along with 5-chlorothiophenyl moiety was found to have the most potent inhibitory effect on the production of ROS in LPS-stimulated RAW 264.7 macrophages with an IC50 value of 3.29??M.