ANTI-TUMOR ACTIVITY OF SOME CYCLOPHOSPHAZENES

被引:62
作者
LABARRE, JF [1 ]
FAUCHER, JP [1 ]
LEVY, G [1 ]
SOURNIES, F [1 ]
CROS, S [1 ]
FRANCOIS, G [1 ]
机构
[1] CNRS,PHARMACOL & TOXICOL FONDAMENTALES LAB,F-31400 TOULOUSE,FRANCE
关键词
D O I
10.1016/0014-2964(79)90137-3
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
Among six cyclophosphazenes tested for antitumour activity against mouse P388, L1210 and B16 tumours respectively, activity was shown by the hexaziridinocyclotriphosphazene (N3P3Az6; all three tumours), the octaziridinocyclotetraphosphazene (N4P4Az8; all three tumours) and the octapyrrolidinocyclotetraphosphazene (N4P4Pyrro8; P388 tumour). The most effective in each case is the hexaziridino trimer compound, N3P3Az6, which has the advantage of high water solubility and activity both by the i.v. and by the i.p. route. Three compounds, N3P3Cl6, N4P4Cl8 and N3P3Pyrro6 were inactive. The mode of action of these drugs on DNA and a possible structure-activity relationship are briefly discussed. © 1979.
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收藏
页码:637 / 643
页数:7
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