| Summary: | 碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所 === 98 === This thesis describes synthesis and antiproliferative evaluation of naphtho[2,3-b]furan-4,9-dione derivatives. A number of substituents have been introduced on the N-1, C-2, or C-4 position to investigate the antiproliferative structure activity relationship with respect to the kind of substituents and the position of substitution. Preliminary results indicated that (E)-1-cyclopropyl-4,9-dioxo-4,9-dihydro-naphtho[2,3-d]imidazole- 2-carbaldehyde O-2-(piperidin-1-yl)ethyl oxime (20), (Z)-N-(4-(1-ethyl-2-methyl-9-oxo-naphtho[2,3-d]imidazol-ylideneamino- phenyl)acetamide (21d), and (Z)-4-(1-cyclopropyl-2-methyl-9-oxo- naphtho[2,3-d]imidazol-ylideneamino)-N-(2-(diethylamino)ethyl)benzamide (21e) , 1-(3-(Dimethylamino)propyl)-2-(furan-2-yl)-1H-naphtho[2,3-d]imidazole -4,9- dione (25e) exhibited selective inhibitory activity against the growth of A549 cancer cell line with GI50 value of 6.40, 6.93, and 6.48 ?嵱 respectively. Compound (25e) of the CE81T cell lines GI50 value is 4.78μM
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