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Antitumor activity of the R- and S-enantiomers of RS-2-[[hydroxy[[2-[
W J Houlihan1, K Prasad, R Underwood
1Sandoz Research Institute, Sandoz Pharmaceuticals Corporation, East Hanover, New Jersey 07936, USA.
Journal of Medicinal Chemistry
|January 19, 1996
Abstract:
The R- and S-enantiomers of 2-[[hydroxyl[[2-[(octadecyloxy) methyl]tetrahydrofuran-2-yl]methoxy]-phosphinyl]oxy]-N,N,N,- trimethylethylaminium hydroxide salt (SRI 62-834) have been evaluated in several assays to determine potential antitumor activity. The S-enantiomer showed slightly greater cytotoxic activity than the R- or RS-forms against several murine tumor cell lines. In the mouse Meth A fibrosarcoma model, the S-enantiomer was ca. 4 times more effective than the R-isomer in controlling size of tumor growth and increasing the number of survivors.