| Literature DB >> 21334116 |
Xiaojian Wang1, Na Lu, Qian Yang, Dandan Gong, Changjun Lin, Shenglie Zhang, Meiyang Xi, Yuan Gao, Libing Wei, Qinglong Guo, Qidong You.
Abstract
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 anti-tumor activity as GA. Mechanistic studies on 11a determined that the compound induces apoptosis as well as arrests the G2/M phase of the cell cycle in HepG2 cells. The determination of the essential part of the scaffold found in GA to maintain anti-tumor effects, and the SAR based on the caged pharmacophore are reported and will provide key information for future anti-cancer drug development studies.Entities:
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Year: 2011 PMID： 21334116 DOI： 10.1016/j.ejmech.2011.01.051
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514