Antitumor Activity of the R- and S-Enantiomers of RS-2-[[Hydroxy[[2-[(octadecyloxy)methyl]tetrahydrofuran-2-yl]methoxy]phosphinyl]oxy]-N,N,N-trimethylethylaminium Hydroxide Inner Salt

The R- and S-enantiomers of 2-[[hydroxy[[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 ac...

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Veröffentlicht in:Journal of medicinal chemistry 1996-01, Vol.39 (2), p.605-608
Hauptverfasser: Houlihan, William J, Prasad, Kapa, Underwood, Russell, Repič, Oljan, Munder, Paul G
Format: Artikel
Sprache:eng
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Zusammenfassung:The R- and S-enantiomers of 2-[[hydroxy[[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 the size of tumor growth and increasing the number of survivors.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm950072e