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

Authors :
Shujian Hu
Junyi Wang
Xiao-Jun Yao
Yunhao Ma
Peng Chen
Hao Zhang
Xinrong Jiang
Wantong Ma
Hongyuan Tu
Kangjia Du
Mengze Sun
Zhongkun Zhou
Xiaoliang Tang
Rentao Zhang
Source :
European journal of pharmacology. 915
Publication Year :
2021

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 (IC50) 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 (LD50) 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.

Details

ISSN :
18790712
Volume :
915
Database :
OpenAIRE
Journal :
European journal of pharmacology
Accession number :
edsair.doi.dedup.....4f93f464e49be4774e8d8cff0aabf071