Inhibition of LPS-stimulated ROS production by fluorinated and hydroxylated chalcones in RAW 264.7 macrophages with structure-activity relationship study |
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Authors: | Ganesh Bist Nirmala Tilija Pun Til Bahadur Thapa Magar Aarajana Shrestha Hye Jin Oh Amrita Khakurel Pil-Hoon Park Eung-Seok Lee |
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Institution: | College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea |
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Abstract: | Based on the importance of the previous fluorinated and/or hydroxylated chalcones studies, thirty-six compounds were designed as phenyl or hydroxyphenyl bearing fluoro, trifluoromethyl or trifluoromethoxy phenyl propenones and synthesized by applying modified Claisen-Schmidt condensation reaction as a single step. Inhibitory effects of the synthesized compounds on ROS production stimulated by LPS in RAW 264.7 macrophage were evaluated. Structure-activity relationship (SAR) study revealed that the compounds possessing para-hydroxyphenyl group combined with meta-fluoro or meta-trifluoromethyl phenyl group, and meta/para-hydroxyphenyl group combined with ortho-trifluoromethoxyphenyl group have an essential role in inhibiting the LPS-stimulated ROS production in RAW 264.7 macrophages. The most significant inhibitory effect on LPS-stimulated ROS production in RAW 264.7 macrophages was observed in compound 30 that possessed para-hydroxyphenyl group along with ortho-trifluoromethoxyphenyl group. |
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Keywords: | Fluorinated and hydroxylated chalcones Inhibition of LPS-stimulated ROS production SAR study |
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