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Updated: Aug 8, 2026

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
Investigation into the structure-activity relationship of novel concentration dependent, dual action T-type calcium
William F McCalmont1, Jaclyn R Patterson, Michael A Lindenmuth
1Department of Chemistry, University of Virginia, Charlottesville, VA 22904-4319, USA. wfm3s@virginia.edu
Abstract:
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.
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