中文摘要：

Gambogic 酸(GA， 1 ) ， Garcinia 自然产品的最突出的代表，被报导了是一个有希望的反肿瘤代理人。为了推进，探索 GA 的结构活动关系并且作为反肿瘤代理人发现新奇 GA 衍生物， 17 新奇 C-37 修改了 GA 的衍生物被综合并且评估为他们的在里面对 A549， HCT-116， BGC-823， HepG2 和 MCF-7 的 vitro 反肿瘤活动癌症房间线。在他们之中， 11 混合物被发现比对一些癌症房间线的 GA 是更多的有势力。尤其是，化合物 8 是比对有 0.12 的 IC50 价值的 A549 和 BGC-823 房间线的 GA 更活跃的几乎 510 褶层 ??????????????????? ????? 獩煯極潮楬敮 ?? 崀? 嵠吗？？

英文摘要：

Gambogic acid （GA, 1）, the most prominent representative of Garcinia natural products, has been reported to be a promising anti-tumor agent. In order to further explore the structure-activity relationship of GA and discover novel GA derivatives as anti-tumor agents, 17 novel C-37 modified derivatives of GA were synthesized and evaluated for their in vitro anti-tumor activities against A549, HCT-116, BGC-823, HepG2 and MCF-7 cancer cell lines. Among them, 11 compounds were found to be more potent than GA against some cancer cell lines. Notably, com- pound 8 was almost 5--10 folds more active than GA against A549 and BGC-823 cell lines with the IC50 values of 0.12 μmol·L^-1 and 0.57 μmol·L^-1, respectively. Chemical modification at C-37 position of GA by introducing of hydrophilic amines could lead to increased activity and improved drug-like properties. These findings will enhance our understanding of the structure-activity relationship （SAR） of GA and lead to the discovery of novel GA derivatives as potential anti-tumor agents.