Synthesis and anticancer evaluations of novel 1H-imidazole [4,5-f][1,10] phenanthroline derivative for the treatment of colorectal cancer
Document Type
Article
Publication Date
8-5-2022
Abstract
1H-imidazole [4,5-f][1,10] phenanthroline is a promising chemical structure for cancer treatment. Herein, we synthesized a novel 1H-imidazole [4,5-f][1,10] phenanthroline derivative named IPM714 and found it exhibited selectively colorectal cancer (CRC) cells inhibitory activities, with half maximal inhibitory concentration (IC50) of 1.74 μM and 2 μM in HCT116 cells and SW480 cells, respectively. The present study is intended to explore the cytotoxicity of IPM714 in cancer cells of various types and its anticancer mechanism in vitro. Cellular functional analyses indicated IPM714 can arrest HCT116 cell cycle in S phase and induce apoptosis in HCT116 and SW480 cells. Western blot and molecular docking showed that IPM714 may suppress PI3K/AKT/mTOR pathway to inhibit cell proliferation and regulate cell cycle as well as apoptosis. This study proved IPM714 to be a promising drug in CRC therapy.
Publication Title
European Journal of Pharmacology
DOI
10.1016/j.ejphar.2022.175120
Recommended Citation
Hu, Shujian; Ma, Wantong; Wang, Junyi; Ma, Yunhao; Zhou, Zhongkun; Zhang, Rentao; Du, Kangjia; Zhang, Hao; Sun, Mengze; Jiang, Xinrong; Tu, Hongyuan; Tang, Xiaoliang; Yao, Xiaojun; and Chen, Peng, "Synthesis and anticancer evaluations of novel 1H-imidazole [4,5-f][1,10] phenanthroline derivative for the treatment of colorectal cancer" (2022). Kean Publications. 567.
https://digitalcommons.kean.edu/keanpublications/567