Synthesis and antitumor activity of 3-methyl-4-oxo-3,4-dihydroimidazo [5,1-d][1,2,3,5]tetrazine-8-carboxylates and -carboxamides.
Molecules, 2010/12/20;15(12):9427-37.
Liu D[1], Yang JG, Cheng J, Zhao LX
Affiliations
PMID: 21173727DOI: 10.3390/molecules15129427
Impact factor: 4.927
Abstract
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 μg/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.
MeSH terms
Antineoplastic Agents; Dacarbazine; Drug Screening Assays, Antitumor; HL-60 Cells; Heterocyclic Compounds, 2-Ring; Humans; Neoplasms; Solubility; Temozolomide; Water
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