Design, synthesis, and biological evaluation of novel T-Type calcium channel antagonists
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- 作者：McCalmont ; William F. ; Heady ; Tiffany N. ; Patterson ; Jaclyn R. ; Lindenmuth ; Michael A. ; Haverstick ; Doris M. ; et. al.
- 关键词：Calcium channel blockers ; Cancer ; T-type calcium channels ; Cellular proliferation
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2004
- 出版时间：July 16, 2004
- 年：2004
- 卷：14
- 期：14
- 页码：3691-3695
- 全文大小：273 K
文摘
This paper describes the synthesis of several novel T-type calcium channel antagonists that inhibit calcium influx into the cell, which in turn regulates unknown aspects of the cell cycle pathway that are responsible for cellular proliferation. A library of compounds was synthesized anda brief structure activity relationship will be described. From these studies we have identified a compound (1) that displays anti-proliferative activity in the low micromolar range across a variety of cancer cell lines.