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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

1
Pharmaceutical College, Henan University, Kaifeng 475001, China
2
Key Laboratory of Natural Medicine and Immuno-Engineering, Henan University, Kaifeng 475001, China
3
College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475001, China
4
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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Abstract

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
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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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