Synthesis and Biological Evaluation of Furo[3,2-c]quinoline and Furo[2,3-b]quinoline Derivatives

• Main Authors: Hsin-Hsien Lai, 賴心��
• Other Authors: 曾誠齊
• Format: Others
• Language: zh-TW
• Online Access: http://ndltd.ncl.edu.tw/handle/90907098418254836288

碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所碩士班 === 94 === The tricyclic furo[2,3-b]quinoline skeleton constitutes an important group of bioactive natural products such as dictamnine, acrophylline, confusameline, skimmianine, kokusaginine, and haplopine. These alkaloids were found to possess wide-ranging biological properties including anti-allergic, anti-inflammatory, cytotoxic, antiplatelet aggregation, and the voltage-gated potassium channel blocking activities. Due to the biological versatility of furo[2,3-b]quinoline derivatives, we have synthesized a number of linear furo[2,3-b]quinoline derivatives with cyclic amino moiety substituted at C-4 position for antiproliferative evaluation. In order to establish structure-activity relationship (SAR), we have also synthesized certain isomeric angular furo[3,2-c]quinoline derivatives for comparison. The preliminary assay indicated these compounds did not significantly inhibit the growth of MCF7, NCI-H460, and SF-268 at a concentration of 4 μg/ml. Their anti-inflammatory and anti-platelet activities will also be evaluated.