Synthetic Optimization of Ellipticine and Antitumor Activity of Novel Hexacyclic Derivatives of Ellipticine

(E-pub Ahead of Print)

Author(s): Jingjing Lin, Mei Tang, Ru Zhao, Qianqian Du, Longying Shen, Guohua Du, Yafen Zhang, Yan Li*, Xiandao Pan*.

Journal Name: Current Pharmaceutical Design

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A high-yield synthetic procedure of ellipticine has been optimized, and the total yield was up to 50% without silica gel column chromatography. Novel hexacyclic ellipticine derivatives were synthesized by coupling ellipticine with o-aminobenzoic acid. Their cytotoxicities against HCT116, MGC803, HT29 and MCF-7 tumor cells were evaluated. Compound 1a, 1k, 1l showed cytotoxic activity comparable to that of ellipticine. The study of in vivo antitumor activity showed that derivative 1l possessed significant growth inhibitory effect against two types of mouse tumor models and a human lung cancer xenograft model. The anti-tumor effect of compound 1l was better than that of ellipticine, and could arrest cell cycle at the G2 phase and induced late apoptosis in lung cancer cells analyzed by FCM. The study of the mechanism of action suggested that 1l might be a topoisomerase IIα inhibitor.

Keywords: Ellipticine, Hexacyclic derivatives, Synthesis, Antitumor activity, Topoisomerase IIα inhibitor

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(E-pub Ahead of Print)
DOI: 10.2174/1381612825666190404122650
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