Relationship between the chemical structures and biological activities (toxicity, mutagenic and antitumor) in newly synthesized derivatives of pyrazolo pyrimidines.
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.
Nersesyan
A
A
National Center of Oncology, Yerevan, Armenia. armen.nersesyan@meduniwien.ac.at
Muradyan
R
R
Arsenyan
F
F
Danagulyan
G
G
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D001854:Bone Marrow Cells / Q000187:drug effects; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy*; D005260:Female; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D048629:Micronuclei, Chromosome-Defective / Q000139:chemically induced*; D015162:Micronucleus Tests; D015394:Molecular Structure; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D011720:Pyrazoles; D011743:Pyrimidines