New designs and structure activity relationships in antitumoral aziridinyl cyclophospha(thia)zenes |
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Authors: | J C Van De Grampel A A Van Der Huizen A P Jekel J W Rusch T Wilting W Akkerman |
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Institution: | 1. Departments of Inorganic Chemistry , University of Groningen Rijswijk , Nijenborgh 16, 9747, AG Groningen, The Netherlands;2. University of Groningen Rijswijk, Department of Inorganic Chemistry , Nijenborgh 16, 9747, AG Groningen, The Netherlands |
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Abstract: | Abstract The partial aziridinolysis of (NPCl2)3,4 and (NPCl2)2 NSOCl yields non-geminal and geminal chloro-aziridinyl derivatives. Compounds N3P3Az6-nRn (Rdbnd]amino, alkoxy, aryloxy, id.) show in vitro and in vivo cytostatic activity. Structure-activity relationships are proposed. Phase I clinical trials of (NPAz2)2 NSOAz (Azdbnd]1-aziridinyl) are summarized. |
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