1-아릴옥시메틸-2,4,5-트리플루오로벤젠 유도체의 합성 및 CCL2 발현의 억제 활성

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. KCI Citation Count: 0