中文摘要：

4-喹诺酮结构由于其化学易合成性和生物体内潜在的多功能性,使其成为药物化学研究的热门优势结构之一。近年来,4-喹诺酮类成为抗肿瘤药物设计的新方向,已经报道了很多具有抗肿瘤活性的新型4-喹诺酮化合物,主要包括拓扑异构酶Ⅱ、拓扑异构酶Ⅰ、G-四链体、微管蛋白、CK2蛋白激酶受体以及JAK-STAT3信号转导通路等,这些新型4-喹诺酮类化合物对肿瘤细胞的作用靶点新颖多样。该文简述了4-喹诺酮骨架的构建方法,重点介绍近年来4-喹诺酮类化合物抗肿瘤活性及其构效关系等方面的最新研究进展。

英文摘要：

Quinolones are among the most common frameworks present in the bioactive molecules and hence represent an attractive starting point for the design of the combinatorial libraries. This review focuses on the 4-quinolone motif as a privileged structure in medicinal chemistry. In the last years,4-quinolones have been reported as antitumor agents targeting on topoisomerase I and U, G-quadruplexes, tubulin, protein kinase CK2 and transcription-3 signaling pathway（ STAT3 ）. Data on the synthetic approaches and structure-activity relationships of 4-quinolones possessing antitumor activities are presented.