Investigation into the structure-activity relationship of novel concentration dependent, dual action T-type calcium channel agonists/antagonists
Investigation into the structure-activity relationship of novel concentration dependent, dual action T-type calcium channel agonists/antagonists
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DOI：
10.1016/j.bmc.2005.03.004
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发表时间：
2005-06-01
影响因子：
3.5
通讯作者：
MacDonald, TL
中科院分区：
文献类型：
--
作者：
McCalmont, WF;Patterson, JR;MacDonald, TL
本文介绍了本课题组前期合成的化合物(1)的一系列直链类似物的合成和生物活性。这些化合物是T型钙通道拮抗剂，对多种癌细胞表现出强大的抗增殖活性。这些类似物对各种癌细胞的结构-活性关系为这一系列化合物提供了一个合理的药效团。此外，这一系列化合物本身也是一组新型的、浓度依赖的、双重作用的T型钙通道激动剂/拮抗剂。(C)2005爱思唯尔有限公司。保留所有权利。
This paper describes the synthesis and biological evaluation of a series of straight chain analogs of a compound (1) that was previously synthesized in our research program. These compounds, which are T-type calcium channel antagonists, exhibits potent anti-proliferative activity against a variety of cancer cells. A structure-activity relationship of these analogs against a variety of cancer cells has provided insight into a logical pharmacophore for this series of compounds. Furthermore, this series of compounds has presented itself as a set of novel, concentration dependent, dual action agonists/antagonists for the T-type calcium channel. (c) 2005 Elsevier Ltd. All rights reserved.