Xie Lijuan, Qian Xuhong, Cui Jingnan, Xiao Yi, Wang Kewei, Wu Peichun, Cong Liying
State Key Laboratory of Fine Chemicals, Dalian University of Technology, PO Box 89, Zhongshan Road 158, Dalian 116012, China.
Bioorg Med Chem. 2008 Sep 15;16(18):8713-8. doi: 10.1016/j.bmc.2008.07.081. Epub 2008 Aug 3.
A series of novel N-substituted angular furoquinolinone derivatives were synthesized and evaluated for their antitumor activities against QGY, K562, HeLa, P388, and A549 cell lines in vitro. The derivatives bearing basic amino side chain showed an improved antitumor activity. Compound 5h N-(2-dimethylamino-ethyl)-2-(4,8,9-trimethyl-2-oxo-2H-furo[2,3-h]quinolin-1-yl)-acetamide exhibited the highest activities against P388 and A549 cell lines, which are evidenced by the IC(50) values that are four to five fold lower than that for unsubstituted parent compound. DNA-binding experiments suggested that these derivatives bind to DNA through intercalation.
合成了一系列新型N-取代角型呋喃喹啉酮衍生物，并对其体外抗QGY、K562、HeLa、P388和A549细胞系的抗肿瘤活性进行了评估。带有碱性氨基侧链的衍生物显示出增强的抗肿瘤活性。化合物5h N-(2-二甲基氨基乙基)-2-(4,8,9-三甲基-2-氧代-2H-呋喃并[2,3-h]喹啉-1-基)乙酰胺对P388和A549细胞系表现出最高活性，IC(50)值比未取代母体化合物低四至五倍，证明了这一点。DNA结合实验表明，这些衍生物通过插入作用与DNA结合。
