Jiang Nan, Zhai Xin, Chen Zhichao, Liang Chuang, Sun Chao, Han Jing, Gong Ping
Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, P. R. China.
Chem Pharm Bull (Tokyo). 2012;60(5):659-64. doi: 10.1248/cpb.60.659.
With an aim to develop promising anti-tumor agents, a novel series of 2-arylvinyl-4-aminoquinoline derivatives were designed, synthesized and evaluated for their cytotoxicity against H-460, HT-29, HepG2 and SGC-7901 cell lines in vitro. The pharmacological results indicated that most compounds were more potent than the positive controls, especially compounds 8, 14 and 16 with IC(50) values ranging from 0.05 to 0.85 µM against all tested cell lines respectively, which were 5.7- to 112-fold better than Iressa. The most active compound 14 (IC(50) values of 0.05, 0.25, 0.16, 0.68 µM), bearing 4-fluorostyryl at C-2 position and 3-(dimethylamino)-1-propylamino at C-4 position, showed great promise as a lead for the development of more effective quinoline analogues.
为了开发有前景的抗肿瘤药物，设计、合成了一系列新型的2-芳基乙烯基-4-氨基喹啉衍生物，并对其体外抗H-460、HT-29、HepG2和SGC-7901细胞系的细胞毒性进行了评估。药理结果表明，大多数化合物比阳性对照更有效，尤其是化合物8、14和16，它们对所有测试细胞系的IC(50)值分别为0.05至0.85 μM，比易瑞沙（Iressa）好5.7至112倍。活性最高的化合物14（IC(50)值为0.05、0.25、0.16、0.68 μM），在C-2位带有4-氟苯乙烯基，在C-4位带有3-(二甲基氨基)-1-丙基氨基，作为开发更有效喹啉类似物的先导物显示出巨大潜力。
