期刊
HETEROCYCLES
卷 88, 期 1, 页码 663-673出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.3987/COM-13-S(S)20
关键词
Loperamide; Antiproliferative Activity; Opioid; Apoptosis; Caspase-3
资金
- Japan Society for promotion of Science (JSPS) [23590143]
- Grants-in-Aid for Scientific Research [24590040] Funding Source: KAKEN
The structure of 4-arylpiperidin-4-ol, a constituent of the antidiarrheal loperamide, is key to v. opioid receptor activation. Some opioid derivatives were recently reported to induce tumor cell death, but the chemical structures responsible for their antitumor activity remain unclear. We synthesized loperamide analogs and tested their antiproliferative activity against HCT-116 colon tumor cells and HL-60 leukemia cells. The N-substituents on 4-arylpiperidin-4-ol units were found to play an important role in their antiproliferative activity, and the N-diphenylpropanol analogs exhibited the most potent antiproliferative activity. Furthermore, the N-diphenylpropanol analog activated caspase-3, as was found previously for opioids that exhibited antitumor effects.
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