Synthesis and antitumor activity of s-tetrazine derivatives.
Fifty-five compounds of s-tetrazine derivative including hexahydro-, 1,6-dihydro, 1,4-dihydro-, 1,2-dihydro- and aromatic s-tetrazine were prepared. Their antitumor activities were evaluated in vitro by MTT method for P-388 cell and SRB method for A-549 cell. The results show that there are 9 compounds which in 10(-6) microM have more than 50% inhibition rate to A-549 cancer cell growth, and 7 compounds in 10(-6) microM have more than 50% inhibition rate to P-388 cancer cell growth. The IC(50) of compound 3q for P-388, Bel-7402, MCF-7 and A-549 are 0.6 microM, 0.6 microM, 0.5 microM and 0.7 microM, respectively. So s-tetrazine derivative is a kind of compound which possesses potential antitumor activities and is worth to research further.
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China. huyang@mail.hz.zj.cn
Wei-Xiao
WX
Hu
Guo-Wu
GW
Rao
Ya-Quan
YQ
Sun
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D007941:Leukemia P388; D051379:Mice; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D013777:Tetrazoles