%0 Journal Article
%T Synthesis and Antitumor Activity of 3-Methyl-4-oxo-3,4-dihydroimidazo [5,1-d][1,2,3,5]tetrazine-8-carboxylates and -carboxamides
%A Dan Liu
%A Jian-Guo Yang
%A Jie Cheng
%A Lin-Xiang Zhao
%J Molecules
%D 2010
%I MDPI AG
%R 10.3390/molecules15129427
%X Seventeen novel 3-methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylate and -carboxamide derivatives were synthesized and evaluated for their growth inhibition in seven human solid tumor and a human leukemia HL-60 cell lines. Compound IVa showed more activity than the other compounds and the positive control temozolomide. In the presence of 40 mg/mL of IVa, the survival rate of all tested tumor cells was less than 10%. Esters displayed more potent antitumour activity than amides and temozolomide against HL-60 cells. These compounds also exhibited considerably enhanced water-solubility.
%K antitumour activity
%K 3-methyl-4-oxo-3
%K 4-dihydroimidazo[5
%K 1-d][1
%K 2
%K 3
%K 5]-tetrazine-8-carboxylates
%K 3-methyl-4-oxo-3
%K 4-dihydroimidazo[5
%K 1-d][1
%K 2
%K 3
%K 5]tetrazine-8-carboxamides
%K synthesis
%U http://www.mdpi.com/1420-3049/15/12/9427