噻唑并嘧啶类衍生物的设计合成及抗肿瘤活性研究

Design and Synthesis of Thiazolopyrimidine Derivatives and Their Antitumor Activities

为了发现具有良好抗肿瘤活性的新型先导化合物,在综合分析多种高活性化合物结构特点的基础上,设计、合成了一系列含噻唑并[3,2-a]嘧啶-5-酮类化合物。以6-氨基-2-硫脲嘧啶为原料,经4步反应制得目标化合物,其结构经IR,1 H NMR,13C NMR和HRMS确证,并对该类化合物合成影响因素和结构特点进行了探讨。采用噻唑蓝(MTT)法测试了所合成化合物的体外抗肿瘤(A549,MCF-7)活性,测试结果表明大部分化合物对于所试验的癌细胞的增殖都有一定程度的抑制作用。

To find new lead compounds with antitumor activities, a series of novel thiazolo[3,2-α]pyrimi din-5-ones were designed on the base of the reported active compounds. The target compounds were synthesized from 6 amino 2 thiouracils in 4 steps and the main factors affecting the reactions of synthesis were investigated. Their structures were confirmed by IR, ^1H NMR, ^13C NMR and HRMS. The activities of the target compounds against two cancer cell lines （A549, MCF-7） were evaluated by methyl thiazolyl tetrazolium （MTT） in vitro. The preliminary bioassay results indicated that most of the target compounds exhibited potent antitumor activities.