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Molecules 2016, 21(12), 1637;

Synthesis and Biological Evaluation of Novel Aromatic Imide-Polyamine Conjugates

Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, China
Pharmaceutical College, Henan University, Kaifeng 475001, China
College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475001, China
Key Laboratory of Natural Medicine and Immuno-Engineering, Kaifeng 475001, China
Authors to whom correspondence should be addressed.
Academic Editors: Derek J. McPhee and Bimal K. Banik
Received: 1 October 2016 / Revised: 17 November 2016 / Accepted: 23 November 2016 / Published: 30 November 2016
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [1950 KB, uploaded 30 November 2016]   |  


Three types of conjugates in which aromatic imide scaffolds were coupled to diverse amine/polyamine motifs were synthesized, and their antitumor activities were evaluated in vitro and in vivo. Results showed that the conjugate 11e of 1,8-naphthilimide with spermine had pronounced effects on inhibiting tumor cell proliferation and inducing tumor cell apoptosis via ROS-mediated mitochondrial pathway. The in vivo assays on three H22 tumor transplant models revealed that compound 11e exerted potent ability in preventing lung cancer metastasis and extending lifespan. Furthermore, the efficacy of 11e in inhibiting tumor growth and improving body weight index were better than that of positive control, amonafide. Our study demonstrates that compound 11e is a valuable lead compound for further investigation. View Full-Text
Keywords: naphthalimide; polyamine; antitumor; synthesis; amonafide naphthalimide; polyamine; antitumor; synthesis; amonafide

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Li, M.; Wang, Y.; Zhang, J.; Xie, S.; Wang, C.; Wu, Y. Synthesis and Biological Evaluation of Novel Aromatic Imide-Polyamine Conjugates. Molecules 2016, 21, 1637.

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