Studies on the Synthesis and Biological Activities of Furo[3,2-c]quinoline Derivatives

• Main Authors: Hao-Tang Chiang, 蔣浩堂
• Other Authors: Cherng-Chyi Tzeng
• Format: Others
• Language: zh-TW
• Published: 2004
• Online Access: http://ndltd.ncl.edu.tw/handle/77765232281054811928

碩士 === 高雄醫學大學 === 醫藥暨應用化學系碩士班 === 92 === The quinoline alkaloids isolated from the Rutaceac family of plants have various biological activities such as anticancer, antibacterial and antiviral effects. Polycondensed heterocyclic aromatic compounds having a planar structure can intercalate into DNA to inhibit the replication. We have synthesized the derivatives of furoquinoline by changing the substitutent at C4, such as aniline group and aliphatic amines, to improve the selectivity and specificity of the compounds against the growth of various cancer cells. The furo[3,2-c]quinolin-4-yl-(3-methoxyphenyl)amine (51), 3-(furo[3,2-c]quinolin-4-ylamino)phenol (54), 4-(furo[3,2-c]quinolin-4- ylamino)phenol (55) and (4-fluorophenyl)furo[3,2-c]quinolin-4-ylamine (56) exhibit good inhibition on the lung cancer cell NCI-H460, breast cancer cell MCF-7 and CNS cancer cell SF-268. However, the furo[3,2-c]quinolin-4-yl-(2-methoxyphenyl)amine (50), furo[3,2-c]quino- lin-4-yl-(4-methoxyphenyl)amine (52), 2-(furo[3,2-c]quinolin-4-ylamino) phenol (53), (4-chlorophenyl)furo[3,2-c]quinolin-4-ylamine (57) demonstrate good inhibition only on lung cancer cell NCI-H460.