| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1397425 | European Journal of Medicinal Chemistry | 2012 | 12 Pages |
Twenty-six emodin derivatives (17 novel) which attach quaternary ammonium salt were synthesized and evaluated for their anticancer activities in vitro and in vivo. Compounds 11g + 12g and 11h + 12h had more significant antiproliferative ability against three cancer cell lines and low cytotoxicity to HELF. 11g + 12g and 11h + 12h induced AGS cell apoptosis and arrested cell cycle at the G0/G1 phase in a dose-dependent manner. Furthermore, the activities of the caspase-3, -9 enzymes were increased in the treated cells. In vivo studies revealed that compounds 11g + 12g and 11h + 12h showed significant anti-tumor activity compared with controlled group.
Graphical abstractSeventeen new emodin derivatives were synthesized and investigated their anticancer activities. Compounds 11g + 12g and 11h + 12h induced cancer cells apoptosis in vitro and exerted preferable proliferation inhibition effect in vivo.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Twenty-six emodin derivatives (17 novel) were synthesized. ► Compounds 11g + 12g and 11h + 12h showed significant antiproliferative activity in vitro. ► 11g + 12g and 11h + 12h induced apoptosis through caspase-9 and caspase-3 activation. ► 11g + 12g and 11h + 12h arrested cell cycle progression at G0/G1 phase in AGS cells. ► 11g + 12g and 11h + 12h exerted a preferable proliferation inhibition effect in vivo.
