Department of Chemistry, University of Pittsburgh, Pittsburgh, PA 15260, USA
Laboratory of Biochemical Pharmacology, Memorial Sloan Kettering Cancer Center, 1275 York Avenue, New York, NY, 10021, USA
Abstract:
The synthesis and biological evaluation of about one dozen 7-silylcamptothecin derivatives are described. Most new compounds show potencies comparable to or better than camptothecin itself. The best compound, 11-fluoro-10-amino-7-trimethylsilylcamptothecin, is more than 20 times more potent than camptothecin in cell assays.