title: Investigation into the structure-activity relationship of novel concentration dependent, dual action T-type calcium channel agonists/antagonists.
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.
authors.affiliation: Department of Chemistry, University of Virginia, Charlottesville, VA 22904-4319, USA. wfm3s@virginia.edu
authors.forename: William F
authors.initials: WF
authors.lastname: McCalmont
authors.forename: Jaclyn R
authors.initials: JR
authors.lastname: Patterson
authors.forename: Michael A
authors.initials: MA
authors.lastname: Lindenmuth
authors.forename: Tiffany N
authors.initials: TN
authors.lastname: Heady
authors.forename: Doris M
authors.initials: DM
authors.lastname: Haverstick
authors.forename: Lloyd S
authors.initials: LS
authors.lastname: Gray
authors.forename: Timothy L
authors.initials: TL
authors.lastname: Macdonald
mesh_terms: D002120:Calcium Channel Agonists / Q000737:chemistry* / Q000494:pharmacology*; D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology*; D020747:Calcium Channels, T-Type / Q000187:drug effects*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D013329:Structure-Activity Relationship
chemical_list: D002120:Calcium Channel Agonists; D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type