synthesis and antitumor activity of 3-methyl-4-oxo-3,4-dihydroimidazo [5,1-d][1,2,3,5]tetrazine-8-carboxylates and -carboxamides合成与抗肿瘤活性3-methyl-4-oxo-3,4-dihydroimidazo[5,一维][1、2、3、5]tetrazine-8-carboxylates -carboxamides.pdfVIP

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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合成与抗肿瘤活性3-methyl-4-oxo-3,4-dihydroimidazo[5,一维][1、2、3、5]tetrazine-8-carboxylates -carboxamides.pdf

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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合成与抗肿瘤活性3-methyl-4-oxo-3,4-dihydroimidazo[5,一维][1、2、3、5]tetrazine-8-carboxylates -carboxamides

Molecules 2010, 15, 9427-9436; doi: 10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis and Antitumor Activity of 3-Methyl-4-oxo-3,4- dihydroimidazo [5,1-d][1,2,3,5]tetrazine-8-carboxylates and -carboxamides Dan Liu 1, Jian-Guo Yang 2, Jie Cheng 1 and Lin-Xiang Zhao 1,* 1 Key Laboratory of Structure-Based Drugs Design Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China; E-Mails: sammyld@163.com (D.L.); spujack2008@126.com (J.C.) 2 Zhejiang Jinhua CONBA Bio-pharm Co. Ltd., Jinhua 321016, China; E-Mail: yangjg999@163.com (J.-G.Y.) * Author to whom correspondence should be addressed; E-Mail: zhaolinxiang@ (L.-X.Z.); Tel.: (+86)24 Fax: (+86)24 Received: 4 November 2010; in revised form: 10 December 2010 / Accepted: 14 December 2010 / Published: 20 December 2010 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 g/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. Keywords: antitumou