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Synthesis and Antitumor Activity of 3-Methyl-4-oxo-3,4-dihydroimidazo [5,1-d][1,2,3,5]tetrazine-8-carboxylates and -carboxamides

1
Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China
2
Zhejiang Jinhua CONBA Bio-pharm Co. Ltd., Jinhua 321016, China
*
Author to whom correspondence should be addressed.
Molecules 2010, 15(12), 9427-9436; https://doi.org/10.3390/molecules15129427
Received: 4 November 2010 / Revised: 10 December 2010 / Accepted: 14 December 2010 / Published: 20 December 2010
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. View Full-Text
Keywords: antitumour activity; 3-methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]-tetrazine-8-carboxylates; 3-methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamides; synthesis antitumour activity; 3-methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]-tetrazine-8-carboxylates; 3-methyl-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamides; synthesis
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Liu, D.; Yang, J.-G.; Cheng, J.; Zhao, L.-X. 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, 15, 9427-9436.

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