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Synthesis of Cucurbitacin B Derivatives as Potential Anti-Hepatocellular Carcinoma Agents

State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300353, China
Accendatech Company, Ltd., Tianjin 300384, China
Authors to whom correspondence should be addressed.
Molecules 2018, 23(12), 3345;
Received: 12 November 2018 / Revised: 7 December 2018 / Accepted: 14 December 2018 / Published: 18 December 2018
(This article belongs to the Section Medicinal Chemistry)
PDF [1158 KB, uploaded 18 December 2018]


Cucurbitacin B shows potent activity against tumor cells, but its high toxicity limits its application in the clinic. A series of cucurbitacin B derivatives was synthesized and evaluated for their anti-hepatocellular carcinoma (HCC) activities against the HepG-2 cell line. These compounds were also tested for their toxicity against the L-O2 normal cell line. The compound with the most potential, 10b, exhibited potent activity against the HepG-2 cell line with an IC50 value of 0.63 μM. Moreover, compound 10b showed the highest TI value (4.71), which is a 14.7-fold improvement compared to its parent compound cucurbitacin B. A preliminary molecular mechanism study of 10b indicated that 10b could inhibit P-STAT3 to induce the activation of mitochondrial apoptotic pathways. An in vivo acute toxicity study indicated that the compound 10b has preferable safety and tolerability compared with cucurbitacin B. These findings indicate that compound 10b might be considered as a lead compound for exploring effective anti-HCC drugs. View Full-Text
Keywords: Cucurbitacin B; Anti-hepatocellular carcinoma; Derivative; Toxicity; Synthesis Cucurbitacin B; Anti-hepatocellular carcinoma; Derivative; Toxicity; Synthesis

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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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Ge, W.; Chen, X.; Han, F.; Liu, Z.; Wang, T.; Wang, M.; Chen, Y.; Ding, Y.; Zhang, Q. Synthesis of Cucurbitacin B Derivatives as Potential Anti-Hepatocellular Carcinoma Agents. Molecules 2018, 23, 3345.

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