Synthesis and biological activity of a fluorescent schweinfurthin analogue.
Most of the natural schweinfurthins are potent and selective inhibitors of cell growth as measured by the National Cancer Institute's 60-cell line screen. Due to the limited supply of these natural products, we have initiated a program aimed at their synthesis. To date, this effort has led to the preparation of three natural schweinfurthins and more than 40 analogues, and assays on these compounds have afforded some understanding of structure-activity relationships in this family. Further development of schweinfurthins as chemotherapeutic agents would benefit from characterization of their mechanism(s) of action. This perspective led to development of a fluorescent schweinfurthin analogue that retains the differential activity of the natural products, and yet has properties that facilitate its visualization within cells.
Kuder
Craig H
CH
Department of Pharmacology, University of Iowa, Iowa City, IA 52242-1294, USA.
Neighbors
Jeffrey D
JD
Hohl
Raymond J
RJ
Wiemer
David F
DF
D000230:Adenocarcinoma / Q000188:drug therapy; D000972:Antineoplastic Agents, Phytogenic / Q000032:analysis* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D019665:Euphorbiaceae / Q000737:chemistry*; D005456:Fluorescent Dyes / Q000032:analysis* / Q000737:chemistry; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014966:Xanthenes / Q000032:analysis* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D000972:Antineoplastic Agents, Phytogenic; D005456:Fluorescent Dyes; D014966:Xanthenes