Synthesis and biological activity of 1H-imidazo[4,5-f][1,10]phenanthroline as a potential antitumor agent with PI3K/AKT/mTOR signaling

doi:10.1016/j.ejphar.2021.174514

Residential College	false
Status	已發表Published
	Synthesis and biological activity of 1H-imidazo[4,5-f][1,10]phenanthroline as a potential antitumor agent with PI3K/AKT/mTOR signaling
	Hu, Shujian 1; Ma, Wantong 1; Wang, Junyi 2; Zhou, Zhongkun 1; Ma, Yunhao 1; Zhang, Rentao 1; Du, Kangjia 1; Zhang, Hao 1; Sun, Mengze 1; Jiang, Xinrong 1; Tu, Hongyuan 1; Tang, Xiaoliang 3; Yao, Xiaojun 4; Chen, Peng 1
	2022-01-15
Source Publication	European Journal of Pharmacology
ISSN	0014-2999
Volume	915
Abstract	1H-imidazo[4,5-f][1,10]phenanthroline (IPM713) is a type of tricyclic conjugated rigid planar structure with potential medical applications, but its anticancer activity has not yet been fully studied. In the present research, cells from seven different cancer types were used to study the anticancer effect, and IPM713 was found to inhibit the colorectal cancer cell line HCT116 most significantly, with a half maximal inhibitory concentration (IC) of 1.7 μM. The mechanisms by which IPM713 exerts anti-colorectal cancer activity were studied. IPM713 blocked the cell cycle in G0/G1 phase and induced apoptosis by suppressing the PI3K/AKT/mTOR axis. In addition, an acute toxicity test showed that the median lethal dose (LD) was above 5000 mg/kg. The findings of this research suggest that IPM713 can interfere with the PI3K/AKT/mTOR signaling pathway and might be a potential therapeutic candidate for the treatment of colorectal cancer.
Keyword	Apoptosis Cell Cycle Colorectal Cancer Phenanthroline Derivative
DOI	10.1016/j.ejphar.2021.174514
URL	View the original
Indexed By	SCIE
Language	英語English
WOS Research Area	Pharmacology & Pharmacy
WOS Subject	Pharmacology & Pharmacy
WOS ID	WOS:000754688300007
Publisher	ELSEVIER, RADARWEG 29, 1043 NX AMSTERDAM, NETHERLANDS
Scopus ID	2-s2.0-85121420843
Fulltext Access	View Full-Text via DOI View Full-Text via Web of Science View Full-Text via Scopus
Citation statistics
Document Type	Journal article
Collection	University of Macau
Corresponding Author	Chen, Peng
Affiliation	1.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, Macau, Macao
Recommended Citation GB/T 7714	Hu, Shujian,Ma, Wantong,Wang, Junyi,et al. Synthesis and biological activity of 1H-imidazo[4,5-f][1,10]phenanthroline as a potential antitumor agent with PI3K/AKT/mTOR signaling[J]. European Journal of Pharmacology, 2022, 915.
APA	Hu, Shujian., Ma, Wantong., Wang, Junyi., Zhou, Zhongkun., Ma, Yunhao., Zhang, Rentao., Du, Kangjia., Zhang, Hao., Sun, Mengze., Jiang, Xinrong., Tu, Hongyuan., Tang, Xiaoliang., Yao, Xiaojun., & Chen, Peng (2022). Synthesis and biological activity of 1H-imidazo[4,5-f][1,10]phenanthroline as a potential antitumor agent with PI3K/AKT/mTOR signaling. European Journal of Pharmacology, 915.
MLA	Hu, Shujian,et al."Synthesis and biological activity of 1H-imidazo[4,5-f][1,10]phenanthroline as a potential antitumor agent with PI3K/AKT/mTOR signaling".European Journal of Pharmacology 915(2022).

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