Design, Synthesis, and Biological Activity of a Family of Novel Ceramide Analogues in Chemoresistant Breast Cancer Cells

被引：36

作者：

Antoon, James W. ^{[2
,3
]}

Liu, Jiawang ^{[1
]}

Gestaut, Matthew M. ^{[2
,3
]}

Burow, Matthew E. ^{[2
,3
]}

Beckman, Barbara S. ^{[2
,3
]}

Foroozesh, Maryam ^{[1
]}

机构：

[1] Xavier Univ, Dept Chem, New Orleans, LA 70125 USA

[2] Tulane Univ, Sch Med, Dept Pharmacol, New Orleans, LA 70112 USA

[3] Tulane Univ, Sch Med, Dept Med, New Orleans, LA 70112 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 18期

关键词：

CARCINOMA CELLS; RESISTANCE; DEATH; GLUCOSYLCERAMIDE; ACTIVATION; EXPRESSION; PATHWAY;

D O I：

10.1021/jm9009668

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Resistance to chemotherapy and endocrine therapy is a major cause of breast cancer treatment failure. We have synthesized six novel analogues using C8-ceramide as the lead analogue and studied their effect on hormone therapy resistant (MDA-MB-231) and chemoresistant (MCF-7TN-R) breast cancer cells. Pharmacologic intervention using these ceramide analogues inhibited clonogenic survival and induced apoptosis, with one analogue being more effective than C8-ceramide. Our results show ceramide-based therapy has therapeutic potential in treating drug resistant breast cancer.

引用

页码：5748 / 5752

页数：5