Nersesyan A., Muradyan R., Arsenyan F., Danagulyan G.

Relationship between the chemical structures and biological activities (toxicity, mutagenic and antitumor) in newly synthesized derivatives of pyrazolo pyrimidines

Cytology and Genetics 2006, v 40, number 6, 28-32

The relationship between chemical structure, micronucleus-inducing and antitumor activities was studied in four newly synthesized pyrazolo pyrymidine compounds (DGB-216, DGB-227, DGB-228 and DGB-331). In bone marrow erythrocytes of mice no one of compounds was active. Only DGB-216 has slight antitumor activity and increases the mean life span of mice with Ehrlich ascite carcinoma by 11 %, while others were practically non-active. Changes in the chemical structures of the compounds lead to substantial changes in the acute toxicity only. The search of antitumor compounds among the derivatives of -6-etoxycarbonyl-pyrazolo[1,5a]-pyrymidine and -2-methyl-pyrazolo[1,5a]-pyrymidine is useless, as it has been shown in the present investigation. But the search of compounds with antitumor properties among derivatives of pyrazolo pyrymidines is a perspective idea because recently some very active antitumor compounds based on mentioned strusture were synthesized in Italy and the USA.