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Design, synthesis, and biological evaluation of novel T-Type calcium channel antagonists
Authors:McCalmont William F  Heady Tiffany N  Patterson Jaclyn R  Lindenmuth Michael A  Haverstick Doris M  Gray Lloyd S  Macdonald Timothy L
Affiliation:Department of Chemistry, University of Virginia, Charlottesville, VA 22904-4319, USA. wfm3s@virginia.edu
Abstract: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.
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