Design, synthesis, and biological evaluation of novel T-Type calcium channel antagonists
Design, synthesis, and biological evaluation of novel T-Type calcium channel antagonists
复制标题
DOI：
10.1016/j.bmcl.2004.05.011
复制
发表时间：
2004-07-16
影响因子：
2.7
通讯作者：
Macdonald, TL
中科院分区：
文献类型：
--
作者：
McCalmont, WF;Heady, TN;Macdonald, TL
本文描述了几种新型 T 型钙通道拮抗剂的合成，这些拮抗剂抑制钙流入细胞，进而调节负责细胞增殖的细胞周期途径的未知方面。合成了化合物库并描述了简要的结构-活性关系。从这些研究中，我们鉴定出了一种化合物 (1)，它在低微摩尔范围内对多种癌细胞系表现出抗增殖活性。 (C) 2004 Elsevier Ltd. 保留所有权利。
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 and a 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. (C) 2004 Elsevier Ltd. All rights reserved.