Studies on chemical modification and biology of a natural product, gambogic acid (III): determination of the essential pharmacophore for biological activity.

@article{Wang2011StudiesOC,
  title={Studies on chemical modification and biology of a natural product, gambogic acid (III): determination of the essential pharmacophore for biological activity.},
  author={Xiaojian Wang and Na Lu and Qinghua Yang and Dandan Gong and Changjun Lin and Shenglie Zhang and Meiyang Xi and Yuan Gao and Libing Wei and Qinglong Guo and Qidong You},
  journal={European journal of medicinal chemistry},
  year={2011},
  volume={46 4},
  pages={1280-90}
}
Caged 4-oxa-tricyclo[4.3.1.0(3,7)]dec-2-one structural motifs are found in Garcinia natural products that demonstrate anti-tumor activity. Gambogic acid (GA, 1), the most abundant caged Garcinia xanthones, has been reported to be a promising anti-cancer agent. To identify the essential pharmacophore for its anti-tumor activity, a series of GA analogues that address potential key structural features for biological activity were synthesized, among which compound 11a displayed comparable in vitro… CONTINUE READING
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