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백승화,Nakjeong Kim,Seong Hwan Kim,Kwang Hwa Park,정경채,박배근,강남숙 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.1
Androgen receptor (AR) is ligand-inducible nuclear hormone receptor which has been focused on key molecular target in growth and progression of prostate cancer. We synthesized a series of 4-aryl 2-substituted aniline-thiazole analogs and evaluated their anti-cancer activity in AR-dependent human prostate cancer LNCap cells. Among them, the compound 6 inhibited the tumor growth in LNCap-inoculated xenograft model.
4-[(N-Imidazol-2-ylmethyl)anilino]pyranopyridine Analogs as Novel Anti-Angiogenic Agents
오창호,Sun Mi Chae,이규양,Nakjeong Kim,Sunkyung Lee 대한화학회 2005 Bulletin of the Korean Chemical Society Vol.26 No.4
We attempted to replace a benzopyran ring of 4-[(N-imidazol-2-ylmethyl)-4-chloroanilino]benzopyran, previously discovered as anti-angiogenic agent with antitumor activity, with pyranopyridines. The [3,2-c]-, [3,2-b]-, [2,3-c]-, and [2,3-b]-pyranopyridines with N-(imidazol-2-ylmethyl)aniline moiety at the 4-position, were synthesized respectively, and evaluated for primary anti-angiogenic properties through primary cultured HUVEC tube formation assay. From this study, we found that the pyranopyridine ring, especially [3,2-b]- and [2,3-c]-isomer, can replace the benzopyran ring of the compound 1 and can be optimized through the introduction of substituents both on the pyranopyridine ring and the aniline moiety for the identification of a novel anti-angiogenic agent.