新型四唑[1,5-a]并嘧啶-5,7-二醇衍生物的合成及对Cdc25B抑制活性评价

Synthesis and Cdc25B Inhibitory Activity Evaluation of Novel Tetrazolo[1,5-a]Pyrimidin-5,7-diol Derivatives

以5-氨基四唑与丙二酸二乙酯为原料设计并合成了四唑[1,5-a]并嘧啶-5,7-二醇(1)和13个新型6-芳基偶氮四唑[1,5-a]并嘧啶-5,7-二醇(2a~2m)。通过^(1)H NMR,^(13)C NMR,IR,ESI-MS和元素分析等方法对其进行了结构表征。对所合成的目标化合物进行了细胞分裂周期25B磷酸酶(Cdc25B)抑制活性筛选,结果表明:化合物2b,2c,2h,2i和2m对Cdc25B具有抑制作用,其抑制率可高达97.66%。

Tetrazolo[1,5-a]pyrimidin-5,7-diol(1)and thirteen novel tetrazolo[1,5-a]pyrimidin-5,7-diol derivatives(2a~2m)were synthesized in the basis of 5-aminotetrazole and diethyl malonate.The structures of the compounds were characterized by ^(1)H NMR,^(13)C NMR,IR,ESI-MS and elemental analysis.All synthesized target compounds were screened for their inhibitory activity against cell division cycle 25B phosphatase(Cdc25B).The results show that compounds 2b,2c,2h,2i and 2m exhibited good activities against Cdc25B,the inhibition rates up to 97.66%.