Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1341-1345. doi: 10.1016/j.bmcl.2017.02.023.

Jing Yang ¹, Zhengchao Tu ², Xin Xu ¹, Jinfeng Luo ², Xing Yan ¹, Chongzhao Ran ³, Xinliang Mao ¹, Ke Ding ⁴, Chunhua Qiao ⁵

Affiliations

1 College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
2 Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China.
3 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.
4 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.
5 College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China. Electronic address: qiaochunhua@suda.edu.cn.

PMID: 28236592 DOI: 10.1016/j.bmcl.2017.02.023

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.

Keywords

4-Anilinoquinazoline; Anti-cancer agents; Conjugates; EGFR-TKI; Endoperoxide.

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