1380547-17-0Relevant articles and documents
A compound meta-hydroxy phenyl tetrazine dimethyl amide and its preparation and use
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Paragraph 0024; 0025, (2016/11/28)
The invention discloses a new compound, N1,N4-di(3-hydroxyphenyl)-3,6-dimethyl-1,2,4,5-tetrazine-1,4-dicarbonamide shown in formula (I), and preparation and application thereof. The preparation of the compound comprises the steps of using 3,6-dimethyl-1,6-dihydro-1,2,4,5-tetrazine and bis(trichloromethyl) carbonate as raw materials to react with m-hydroxyaniline in an organic solvent in the presence of alkaline catalyst. The compound provided by the invention is applied for preparing medicines for treatment and prevention of human gastric cancer, ovarian cancer, liver cancer, breast cancer or lung cancer. According to the invention, the compound is rational in design, easy in operation, low in production cost and easy to obtain raw materials, and is suitable for industrialized application, and a new choice for screening anti-tumor medicines is provided.
Synthesis, Structure Analysis, and Antitumor Evaluation of 3,6-Dimethyl-1,2,4,5-tetrazine-1,4-dicarboxamide Derivatives
Rao, Guo-Wu,Guo, Yan-Mei,Hu, Wei-Xiao
experimental part, p. 973 - 976 (2012/08/08)
3,6-Dimethyl-1,2,4,5-tetrazine-1,4-dicarboxamide derivatives were synthesized, and their structures were confirmed by single-crystal X-ray diffraction. This reaction yields the 1,4-dicarboxamide derivatives rather than the 1,2-dicarboxamide derivatives. Their invitro antitumor activities were evaluated against SGC-7901, HO-8910, MCF-7, and A-549 cells. The results showed several compounds to be endowed with cytotoxicity in the low micromolar range. One compound (IC50=0.57μM) was further evaluated invivo against an A-549 xenograft in BALB/cA nude mice; it effected 76.4% inhibition of tumor weight through intraperitoneal (i.p.) administration of 40mgkg-1 body weight. Moreover, its acute toxicity was evaluated, and the i.p. LD50 value was 325mgkg-1 in mice.