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 c...

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Published inYaghag-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
LanguageKorean
Published The Pharmaceutical Society Of Korea 30.10.2021
대한약학회
Subjects
약학
CCL2 expression
2
4
5-Trifluorobenzyloxy)benzene
5-Trifluorobenzyloxy)naphthalene
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Summary: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
Bibliography:https://doi.org/10.17480/psk.2021.65.5.370
ISSN:0377-9556
2383-9457
DOI:10.17480/psk.2021.65.5.370