Design, synthesis, and biological evaluation of imidazoline derivatives as p53–MDM2 binding inhibitors

…, W Wang, L Zhang, L Tao, X Dong, R Sheng…

文献索引：Hu, Chunqi; Li, Xin; Wang, Weisi; Zhang, Lei; Tao, Lulu; Dong, Xiaowu; Sheng, Rong; Yang, Bo; Hu, Yongzhou Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 18 p. 5454 - 5461

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被引用次数: 15

摘要

Three series of novel imidazoline derivatives were designed, synthesized, and evaluated for their p53–MDM2 binding inhibitory activities, and anti-proliferation activities against PC3, A549, KB, and HCT116 cancer cell lines. Five of the tested compounds showed enhanced p53–MDM2 binding inhibitory potency and anti-proliferation activities in comparison with that of Nutlin-1. Flow cytometric analysis indicated that compound 7c, one of the most ...