New designs and structure activity relationships in antitumoral aziridinyl cyclophospha(thia)zenes

Abstract
The partial aziridinolysis of (NPCl2)3,4 and (NPCl2)2 NSOCl yields non-geminal and geminal chloro-aziridinyl derivatives. Compounds N3P3Az6-nRn (R[dbnd]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 (Az[dbnd]1-aziridinyl) are summarized.