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

• Published in: Yaghag-hoi-ji Vol. 65; no. 5; pp. 370 - 374
• Main Authors: 김민정(Min Jung Kim), 조아영(Ahyoung Jo), 김관회(Koanhoi Kim), 곽재환(Jae-Hwan Kwak)
• Format: Journal Article
• Language: Korean
• Published: The Pharmaceutical Society Of Korea 30.10.2021; 대한약학회
• Subjects: 약학; CCL2 expression; 2; 4; 5-Trifluorobenzyloxy)benzene; 5-Trifluorobenzyloxy)naphthalene
• DOI: 10.17480/psk.2021.65.5.370
• ISSN: 0377-9556

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