8-氨基苯并呋喃[3,2-d]嘧啶类化合物的合成及其抗癌活性研究  

Synthesis and Antitumor Activities of 8-Aminobenzofuran[3,2-d] Pyrimidine Derivatives

作　　者：杨毓溥 许志玲[2] 卢永仲[3] 王兴东[2] 张前军[1] 

机构地区：[1]贵州大学化学与化工学院,贵阳550025 [2]贵州大学精细化工研究开发中心,贵阳550025 [3]贵州理工学院药学院,贵阳550007

出　　处：《中国药学杂志》2016年第9期690-693,共4页Chinese Pharmaceutical Journal

基　　金：贵州省自然科学基金资助项目(黔科合字[2011]2067号)

摘　　要：目的设计合成8-氨基苯并呋喃[3,2-d]嘧啶类衍生物,并研究其抗癌活性。方法以5-硝基水杨醛为起始原料经过一系列反应合成了目标化合物;采用MTT法评价目标化合物对人结肠癌细胞COLO205、人乳腺癌细胞MCF-7和人白血病细胞K562体外抑制活性。结果合成了9个未见报道的8-氨基苯并呋喃[3,2-d]嘧啶类衍生物,经EI-MS,~1H-NMR,^(13)C-NMR确证其结构。化合物2、3d和5c对COLO205、MCF-7和K562细胞均具有一定的抑制作用,且化合物5c抑制作用尤为明显,在1×10^(-4)mol·L^(-1)浓度下对COLO205、MCF-7和K562细胞的抑制率分别为99.58%,78.75%和98.68%。结论苯并呋喃[3,2-d]嘧啶类衍生物的抗癌活性值得进一步研究。OBJECTIVE To synthesize the derivatives of 8-amino benzofnran[ 3,2-d] pyrimidine and study their anticancer activi- ties. METHODS The target compounds were synthesized through a series of reactions, and their anticancer activities in vitro were e- valuated against COLO205, MCF-7 and K562 cell lines by MTT as assay. RESULTS Nine title compounds were synthesized and confirmed by EI-MS,1H-NMR and 13 C-NMR. Compounds 2, 3d and 5c had good inhibition effect against COLO205, MCF-7 and K562 cells. The inhibition rates of compound 5c against COL0205, MCF-7 and K562 cells were 99.58% ,78.75% and 98.68% respectively at 10-4 mol · L-I. CONCLUSION The anticancer activity of benzofuran[ 3,2-d] pyrimidine derivatives is worthy of further study.

关 键 词：苯并呋喃[3 2-d]嘧啶衍生物 合成 抗癌活性 

分 类 号：R914[医药卫生—药物化学]