新型2-氨基-呋喃并[2,3-d]嘧啶-4(3H)-酮衍生物的合成及抗肿瘤活性

Synthesis and Antitumor Activity of Some 2-Amino-furo[2,3-d]yrimidin-4(3H)-one Derivatives

报道应用aza-Wittig反应,采用易得的原料,在温和的条件下,以78%～90%的产率有效的合成了新型2-氨基-呋喃并[3,2-d]嘧啶-4(3H)-酮衍生物5,其结构经IR,1H NMR,MS和元素分析确认.为进一步得到结构确认,化合物5c经X射线衍射分析证实.运用噻唑蓝(MTT)标准法对化合物5进行了体外抗肿瘤活性的测定,其中5f对肺癌细胞A459的IC50值为18.4μmol/L,显示出潜在良好的抗肿瘤活性.

In this paper,a novel series of 2-aminofuro[2,3-d]yrimidin-4（3H）-one derivatives were prepared via aza-Wittig reaction of iminophosphorane 3 with aromatic isocyanate and subsequent reaction with various amine under mild condition in 78%～90% yields.The structures of these compounds were confirmed by mass spectral data,1H NMR,IR and elemental analysis.Compound 5c was further analyzed by single crystal X-ray diffraction.The in vitro antitumor activities of compounds 5 were analyzed with 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazoliumbromide（MTT） standard method,and compound 5f showed the best inhibition activities against A459 with IC5018.4 μmol/L.