title: Synthesis and Biological Evaluation of Novel Substituted 4-Anilinoquinazolines as Antitumor Agents.
abstract: Eleven novel 4-anilinoquinazoline derivatives were synthesized and evaluated for their in vitro antiproliferative activity. Among them, compound 9a exhibited the best potency, with IC50values of 25-682 nm against various types of cancer cell lines. In addition, 9a was confirmed that it could arrest the cell cycle at G2/M phase and trigger apoptosis. Indirect immunofluorescence staining revealed its antitubulin property. Importantly, 9a significantly inhibited tumor growths in SM-7721 xenograft models (57.0% tumor mass change) without causing significant loss of body weight, suggesting that 9a is a promising new anticancer agent to be developed.
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center of Biotherapy, South of Renmin Road, Chengdu 610041, China.
authors.forename: Dong
authors.initials: D
authors.lastname: Cao
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center of Biotherapy, South of Renmin Road, Chengdu 610041, China.
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center of Biotherapy, South of Renmin Road, Chengdu 610041, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Lei
authors.affiliation: Division of Nephrology, Kidney Research Institute, West China Hospital of Sichuan University, Chengdu, 610041, China.
authors.forename: Liang
authors.initials: L
authors.lastname: Ma
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center of Biotherapy, South of Renmin Road, Chengdu 610041, China.
authors.forename: Zhuang
authors.initials: Z
authors.lastname: Yang
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center of Biotherapy, South of Renmin Road, Chengdu 610041, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, and Collaborative Innovation Center of Biotherapy, South of Renmin Road, Chengdu 610041, China.
authors.forename: Lijuan
authors.initials: L
authors.lastname: Chen
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000473:pathology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013057:Spectrum Analysis / Q000379:methods; D023041:Xenograft Model Antitumor Assays
chemical_list: D000814:Aniline Compounds; D000970:Antineoplastic Agents; D011799:Quinazolines; C000628010:anilinoquinazoline
keywords: 4-anilinoquinazoline derivatives; G2/M arrest; antiproliferation