title: Design, synthesis, and biological evaluation of novel T-Type calcium channel antagonists.
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.
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: Tiffany N
authors.initials: TN
authors.lastname: Heady
authors.forename: Jaclyn R
authors.initials: JR
authors.lastname: Patterson
authors.forename: Michael A
authors.initials: MA
authors.lastname: Lindenmuth
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: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D015764:Bepridil / Q000494:pharmacology; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D020747:Calcium Channels, T-Type / Q000378:metabolism*; D002455:Cell Division / Q000187:drug effects*; D015195:Drug Design; D005069:Evaluation Studies as Topic; D006801:Humans; D020128:Inhibitory Concentration 50; D019169:Jurkat Cells; D010480:Perhexiline / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D015764:Bepridil; D010480:Perhexiline