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KMID : 0370220210650050370
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Yakhak Hoeji
2021 Volume.65 No. 5 p.370 ~ p.374
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Synthesis of 1-Aryloxymethyl-2,4,5-trifluorobenzene Analogs and Their Inhibitory Activity of CCL2 Expressi
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Kim Min-Jeong
Jo Ah-Young
Kim Koan-Hoi
Kwak Jae-Hwan
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Abstract
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CCL2 overexpression is associated with macrophage recruitment during immune response and poor patientprognosis in various cancers, such as prostate, breast, pancreatic, and liver cancer. For developing CCL2 inhibitors, 1-aryloxymethyl-2,4,5-trifluorobenzene analogs were designed and synthesized by concise synthetic route including SN2reaction, reduction, and oxime formation reaction. Furthermore, it was confirmed that they inhibited CCL2 productioninduced by 27-hydroxycholesterol through reverse transcription PCR in the human acute monocytic leukemia cell line(THP-1). Among them, N-((2-(2,4,5-trifluorobenzyloxy)naphthalene-1-yl)methyl)hydroxylamine (4) exhibited the highestCCL2 transcription inhibition activity.
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KEYWORD
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CCL2 expression, (2, 4, 5-Trifluorobenzyloxy)benzene, (2, 4, 5-Trifluorobenzyloxy)naphthalene
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