In our previous work, 3』, 6-substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives were synthesized and evaluated for their anticancer activity. Among these tested compounds, 2-(3-fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3- carboxylic acid (D-1) was the most promising one which was identified as an excellent lead compound and worthy for further investigation. In the present work, D-1 was selected as lead compound, several analogs including I, II, III and IV will be synthesized, The cytotoxicity, action mechanism and antitumor activity of these target compounds will be evaluated. We hope to establish the structure-activity relationships of these compounds and achieve optimization of lead compound D-1.