title: Synthesis and Anti-Tumor Activities of 4-Anilinoquinoline Derivatives.
abstract: Twenty-two 7-fluoro (or 8-methoxy)-4-anilinoquinolines compounds were designed and synthesized as potentially potent and selective antitumor inhibitors. All the prepared compounds were evaluated for their in vitro antiproliferative activities against the HeLa and BGC823 cell lines. Ten compounds (1a-g; 2c; 2e and 2i) exhibited excellent antitumor activity superior to that of gefitinib. Among the ten compounds; seven (1a-c; 1e-1g and 2i) displayed excellent selectivity for BGC823 cells. In particular; 1f and 2i exhibited potent cytotoxic activities against HeLa cells and BGC823 cells with better IC50 values than gefitinib.
authors.affiliation: Department of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China. liudan20040318@163.com.
authors.forename: Dan
authors.initials: D
authors.lastname: Liu
authors.affiliation: Department of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China. sapphire0614@163.com.
authors.forename: Tian
authors.initials: T
authors.lastname: Luan
authors.affiliation: Department of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China. kongjianwm2006@163.com.
authors.forename: Jian
authors.initials: J
authors.lastname: Kong
authors.affiliation: Department of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China. zhingky621@126.com.
authors.forename: Ying
authors.initials: Y
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Engineering, College of Parmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China. 38whf@163.com.
authors.forename: Hai-Feng
authors.initials: HF
authors.lastname: Wang
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D000077156:Gefitinib; D006367:HeLa Cells; D006801:Humans; D011799:Quinazolines / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011799:Quinazolines; D011804:Quinolines; D000077156:Gefitinib
keywords: 4-anilinoquinolines; EGFR; antitumor; inhibitor