title: Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents.
abstract: In the present study, endoperoxide and 4-anilinoqnazoline were conjugated to obtain a series of compounds. These conjugates exhibited high antiproliferative potency against a number of cancer cell lines, including the epidermal growth factor receptor (EGFR) L858R/T790M mutant cell. Compound 5 was selected as a representative for mechanistic study. Further experiments revealed the conjugate's reactive oxygen species (ROS) generating ability, apoptosis inducing activity and involvement in EGFR downstream signaling pathways.
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Yang
authors.affiliation: Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China.
authors.forename: Zhengchao
authors.initials: Z
authors.lastname: Tu
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Xu
authors.affiliation: Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China.
authors.forename: Jinfeng
authors.initials: J
authors.lastname: Luo
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
authors.forename: Xing
authors.initials: X
authors.lastname: Yan
authors.affiliation: Molecular Imaging Laboratory, MGH/MIT/HMS Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital/Harvard Medical School, Building 75, Charlestown, MA 02129, United States.
authors.forename: Chongzhao
authors.initials: C
authors.lastname: Ran
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
authors.forename: Xinliang
authors.initials: X
authors.lastname: Mao
authors.affiliation: Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China. Electronic address: dingke@jnu.edu.cn.
authors.forename: Ke
authors.initials: K
authors.lastname: Ding
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China. Electronic address: qiaochunhua@suda.edu.cn.
authors.forename: Chunhua
authors.initials: C
authors.lastname: Qiao
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D066246:ErbB Receptors / Q000037:antagonists & inhibitors; D006801:Humans; D020128:Inhibitory Concentration 50; D010545:Peroxides / Q000737:chemistry*; D011799:Quinazolines / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D010545:Peroxides; D011799:Quinazolines; D066246:ErbB Receptors
keywords: 4-Anilinoquinazoline; Anti-cancer agents; Conjugates; EGFR-TKI; Endoperoxide