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

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.