期刊
MONATSHEFTE FUR CHEMIE
卷 141, 期 8, 页码 893-899出版社
SPRINGER WIEN
DOI: 10.1007/s00706-010-0337-x
关键词
Apoptosis; Cytotoxicity; Hybrid; Indomethacin; Naphthalimide
资金
- National Natural Science Foundation of China [20536010, 20746003]
- Program of Shanghai Subject Chief Scientist
- Shanghai Leading Academic Discipline Project [B507]
- National High Technology Research and Development Program of China [2006AA10A201]
A series of novel naphthalimide-indomethacin hybrids with different linkers were designed and synthesized. Their antitumor activity was evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8, and A375 cancer cell lines in vitro. Preliminary results showed that the hybrids had moderate cytotoxic activity with 50% inhibition concentration (IC50) values of similar to 10(-5) M, and could effectively induce apoptosis in HeLa cells. More importantly, the amide derivatives had better cytotoxic and proapoptotic activity than their ester counterparts, whereas the ester derivatives had hypoxic preferred cytotoxicity and might be used as promising candidates of prodrug in hypoxic tumor cells. This work provides a novel class of naphthalimide-indomethacin hybrids with unique antitumor activity for further optimization.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据