STUDIES OF SYNTHESES AND ANTITUMOUR ACTIVITY ON 8-TRIAZENOPURINES
- VernacularTitle:8-三氮烯嘌呤类化合物的合成和抗肿瘤活性的研究
- Author:
Wannian ZHANG
- Publication Type:Journal Article
- From:
Academic Journal of Second Military Medical University
1983;0(S1):-
- CountryChina
- Language:Chinese
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Abstract:
In view of the facts that moderately electron withdrowing carrier might cause the triazenes increase antitnmour activity and decrease toxicity, sixteen 8-triaze-nopurines were prepared. 7-H-8-triazenopurines were synthesised by coupling the corresponding 8-diazopurines directly with appropriate secondary amines under carefully controlled conditions, while 7-alkyl-8-triazenotheophyllines were obtained by coupling 8-diazotheophylline with secondary amines to 8-triazenotheophyllmes and subsequent alkylation under suitable conditions.All sixteen compounds have been snbjected to experimental antitumour tests. Preliminary results revealed that compounds 2a, 3a, 4a and 5 possessed marked inhibitory action against L615 in mice and caused ILS of 300-400%, among them compound 4a was was shown to possess the highest activity but less toxicity. The further study is in progress.