| Summary: | 碩士 === 高雄醫學大學 === 藥學研究所 === 99 === The skeleton of natural dictamnine alkaloid belongs to a tricyclic furoquinoline derivative. Previous reports indicated that the introduction of a suitable substituent at the 4-position of furoquinoline ring afforded certain potential antiproliferative agents. For examples, 1-[4-(furo[2,3-b]quinoline-4-ylamino)phenyl]ethanone (1, GI50 = 0.025 μM) and 3-chloro-4-[(4-methoxyphenyl)amino]furo[2,3-b]quinoline (2, GI50 = 0.025 μM) exhibited more potent antiproliferative activities than the clinically used anticancer drug, daunomycin. However, poor water solubility and general cytotoxicities exhibited by both compounds 1 and 2 prompted extensive structural optimizations to overcome these problems. This thesis describes the synthesis and antiproliferative evaluation of certain N-alkyl 4-anilinofuro[2,3-b]quinoline derivatives with an aim to obtain novel furoquinoline derivatives with a high water solubility as well as a better selective anticancer activity. Certain N-alkyl 4-anilinofuro[2,3-b]quinoline derivatives were successfully synthesized and proved to be potential antiproliferative agents.
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