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Synthesis and anticancer evaluations of novel 1H-imidazole [4,5-f][1,10] phenanthroline derivative for the treatment of colorectal cancer
Hu, Shujian1; Ma, Wantong1; Wang, Junyi2; Ma, Yunhao1; Zhou, Zhongkun1; Zhang, Rentao1; Du, Kangjia1; Zhang, Hao1; Sun, Mengze1; Jiang, Xinrong1; Tu, Hongyuan1; Tang, Xiaoliang3; Yao, Xiaojun4; Chen, Peng1
2022-08-05
Source PublicationEuropean Journal of Pharmacology
ISSN0014-2999
Volume928
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 (IC) 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.

Keyword1h-imidazole [4,5-f][1,10] Phenanthroline Apoptosis Cell Cycle Colorectal Cancer Mtor
DOI10.1016/j.ejphar.2022.175120
URLView the original
Indexed BySCIE
Language英語English
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000827400600003
PublisherELSEVIERR, ADARWEG 29, 1043 NX AMSTERDAM, NETHERLANDS
Scopus ID2-s2.0-85132901956
Fulltext Access
Citation statistics
Document TypeJournal article
CollectionUniversity of Macau
Corresponding AuthorChen, Peng
Affiliation1.School of Pharmacy, Lanzhou University, Lanzhou, 199 Donggang West Road, 730000, China
2.College of Science and Technology, Wenzhou-Kean University, Wenzhou, 88 Daxue Road, 325060, China
3.College of Chemistry and Chemical Engineering, Lanzhou University, Lanzhou, 222 Tianshui South Road, 730000, China
4.Macau Institute for Applied Research in Medicine and Health, State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Taipa, Avenida Wai Long, Macao
Recommended Citation
GB/T 7714
Hu, Shujian,Ma, Wantong,Wang, Junyi,et al. Synthesis and anticancer evaluations of novel 1H-imidazole [4,5-f][1,10] phenanthroline derivative for the treatment of colorectal cancer[J]. European Journal of Pharmacology, 2022, 928.
APA 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., & Chen, Peng (2022). Synthesis and anticancer evaluations of novel 1H-imidazole [4,5-f][1,10] phenanthroline derivative for the treatment of colorectal cancer. European Journal of Pharmacology, 928.
MLA Hu, Shujian,et al."Synthesis and anticancer evaluations of novel 1H-imidazole [4,5-f][1,10] phenanthroline derivative for the treatment of colorectal cancer".European Journal of Pharmacology 928(2022).
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