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Molecules 2017, 22(2), 342; doi:10.3390/molecules22020342

Design, Synthesis and Evaluation of Naphthalimide Derivatives as Potential Anticancer Agents for Hepatocellular Carcinoma

Pharmaceutical College, Henan University, Kaifeng 475001, China
Key Laboratory of Natural Medicine and Immuno-Engineering, Henan University, Kaifeng 475001, China
College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475001, China
Institute of Chemical Biology, Henan University, Kaifeng 475001, China
Authors to whom correspondence should be addressed.
Academic Editor: Jean Jacques Vanden Eynde
Received: 13 January 2017 / Revised: 16 February 2017 / Accepted: 16 February 2017 / Published: 22 February 2017
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Two kinds of naphthalimide derivatives were synthesized and evaluated for in vitro their anti-hepatocellular carcinoma properties. Compound 3a with a fused thiazole fragment to naphthalimide skeleton inhibited cell migration of SMMC-7721 and HepG2, and further in vivo trials with two animal models confirmed that compound 3a moderately inhibited primary H22 tumor growth (52.6%) and potently interrupted lung metastasis (75.7%) without obvious systemic toxicity at the therapeutic dose. Mechanistic research revealed that compound 3a inhibited cancerous liver cell growth mostly by inducing G2/M phase arrest. Western blotting experiments corroborated that 3a could up-regulate the cell cycle related protein expression of cyclin B1, CDK1 and p21, and inhibit cell migration by elevating the E-cadherin and attenuating integrin α6 expression. Our study showed that compound 3a is a valuable lead compound worthy of further investigation. View Full-Text
Keywords: synthesis; naphthalimide; hepatocellular carcinoma; cell cycle; lung metastasis synthesis; naphthalimide; hepatocellular carcinoma; cell cycle; lung metastasis

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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Ge, C.; Chang, L.; Zhao, Y.; Chang, C.; Xu, X.; He, H.; Wang, Y.; Dai, F.; Xie, S.; Wang, C. Design, Synthesis and Evaluation of Naphthalimide Derivatives as Potential Anticancer Agents for Hepatocellular Carcinoma. Molecules 2017, 22, 342.

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