The Synthesis and Antitumor Activity of 1,8-Naphthalimide Derivatives Linked 1,2,3-Triazole

Zhong-Jie Xu; Ying-Jie Zhou; Jia-Hao Wang; Long-Fei Mao; Wei Li; Gui-Qing Xu

doi:10.3389/fbioe.2021.662432

The Synthesis and Antitumor Activity of 1,8-Naphthalimide Derivatives Linked 1,2,3-Triazole

Front Bioeng Biotechnol. 2021 Apr 13:9:662432. doi: 10.3389/fbioe.2021.662432. eCollection 2021.

Authors

Zhong-Jie Xu¹, Ying-Jie Zhou², Jia-Hao Wang², Long-Fei Mao², Wei Li², Gui-Qing Xu²

Affiliations

¹ College of Life Science and Technology, Xinxiang Medical University, Xinxiang, China.
² Henan Engineering Research Center of Chiral Hydroxyl Pharmaceutical, School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, China.

Abstract

In this study, acenaphthylene was used as the raw material, and a series of novel 1,8-naphthalimide-1,2,3-triazole derivatives was obtained through oxidation, acylation, alkylation, and click reactions, and subsequently, their anti-tumor activities were tested. After screening, we found that Compound 5e showed good activity against H1975 lung cancer cells, with the half maximal inhibitory concentration (IC₅₀) reaching 16.56 μM.

Keywords: 1,8-naphthalimide-1,2,3-triazole derivatives; H1975; acenaphthylene; anti-proliferative activities; synthesis.