Inorganic ring systems of physiological importance. Part III: Structure and cytostatic activity in vitro of aziridino cyclophospha(thia)zenes
article
The testing for cytostatic activity of a series of 36 aziridino derivatives of (NPCl2)3 and (NPCl2)2NSOCl gives similar results in two different in vitro screening systems. Evaluation of the dose causing 50 per cent inhibition of colony formation (ID50) in mouse leukaemia L1210 cells and the lowest active dose (LAD) established for the radiosensitive mouse lymphoma L5178Y leads to an insight into activating and deactivating structural requirements. The presence of aziridino (N(CH2)2) groups with their alkylating ability and electron releasing substituents is essential for effective tumour growth inhibition. Hydrolytic instability results in loss of gravity.
TNO Identifier
229457
ISSN
00201693
Source
Inorganica Chimica Acta, 78(C), pp. 239-245.
Pages
239-245
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