Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives
AbstractGambogic 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.
Scifeed alert for new publicationsNever miss any articles matching your research from any publisher
- Get alerts for new papers matching your research
- Find out the new papers from selected authors
- Updated daily for 49'000+ journals and 6000+ publishers
- Define your Scifeed now
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.
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(6):6249-6268.Chicago/Turabian Style
Chen, Tao; Zhang, Rong-Hong; He, Shi-Chao; Xu, Qin-Yuan; Ma, Liang; Wang, Guang-Cheng; Qiu, Neng; Peng, Fei; Chen, Jin-Ying; Qiu, Jing-Xiang; Peng, Ai-Hua; Chen, Li-Juan. 2012. "Synthesis and Antiangiogenic Activity of Novel Gambogic Acid Derivatives." Molecules 17, no. 6: 6249-6268.