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RS-2-[[羟基[[2-[(十八烷氧基)甲基]四氢呋喃-2-基]甲氧基]膦酰基]氧基]-N,N,N-三甲基乙铵氢氧化物内盐的R-和S-对映体的抗肿瘤活性

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.

作者信息

Houlihan W J, Prasad K, Underwood R, Repic O, Munder P G

机构信息

Sandoz Research Institute, Sandoz Pharmaceuticals Corporation, East Hanover, New Jersey 07936, USA.

出版信息

J Med Chem. 1996 Jan 19;39(2):605-8. doi: 10.1021/jm950072e.

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.

摘要

2-[[羟基[[2-[(十八烷氧基)甲基]四氢呋喃-2-基]甲氧基]膦酰基]氧基]-N,N,N-三甲基乙铵氢氧化物盐(SRI 62-834)的R-和S-对映体已在多种实验中进行评估,以确定其潜在的抗肿瘤活性。在针对几种小鼠肿瘤细胞系的实验中,S-对映体显示出比R-或RS-形式略强的细胞毒性活性。在小鼠Meth A纤维肉瘤模型中,S-对映体在控制肿瘤生长大小和增加存活数量方面的效果约为R-异构体的4倍。

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