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Molecules 2012, 17(6), 6249-6268; doi:10.3390/molecules17066249

Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives

1, 1, 2, 1, 1, 1, 1, 1, 1, 1, 1 and 1,*
1 State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu, Sichuan 610041, China 2 School of Chemical Engineering, Sichuan University, Chengdu, Sichuan 610065, China
* Author to whom correspondence should be addressed.
Received: 16 April 2012 / Revised: 4 May 2012 / Accepted: 9 May 2012 / Published: 25 May 2012
(This article belongs to the Section Medicinal Chemistry)
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Gambogic acid (GA) is in a phase II clinical trial as an antitumor and antiangiogenesis agent. In this study, 36 GA derivatives were synthesized and screened in a zebrafish model to evaluate their antiangiogenic activity and toxicity. Derivatives 4, 32, 35, 36 effectively suppressed the formation of newly grown blood vessels and showed lower toxicities than GA as evaluated by zebrafish heart rates and mortalities. They also exhibited more potent migration and HUVEC tube formation inhibiting activities than GA. Among them, 36 was the most potent one, suggesting that it may serve as a potential new antiangiogenesis candidate with low toxicity. Additionally, 36 showed comparable antiproliferative activity to HUVECs and five tumor cell lines but low cytotoxicity to LO2 cells.
Keywords: gambogic acid; antitumor; antiangiogenesis; zebrafish; toxicity gambogic acid; antitumor; antiangiogenesis; zebrafish; toxicity
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Chen, T.; Zhang, R.-H.; He, S.-C.; Xu, Q.-Y.; Ma, L.; Wang, G.-C.; Qiu, N.; Peng, F.; Chen, J.-Y.; Qiu, J.-X.; Peng, A.-H.; Chen, L.-J. Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives. Molecules 2012, 17, 6249-6268.

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