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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。
Aim To design and synthesize 8-aminobenzofuran [3,2-d] pyrimidine derivatives and study their anticancer activity. Methods The target compounds were synthesized through a series of reactions using 5-nitrosalicylaldehyde as starting material. The inhibitory activity of the target compounds against human colon cancer cells COLO205, human breast cancer cells MCF-7 and human leukemia K562 cells was evaluated by MTT assay . Results Nine novel 8-aminobenzofuran [3,2-d] pyrimidine derivatives were synthesized and their structures were confirmed by EI-MS, ~ 1H-NMR and ~ (13) C-NMR. Compounds 2, 3d and 5c had certain inhibitory effect on COLO205, MCF-7 and K562 cells, and the inhibitory effect of compound 5c was especially obvious. Under the concentration of 1 × 10 -4 mol·L -1, The inhibitory rates of COLO205, MCF-7 and K562 cells were 99.58%, 78.75% and 98.68%, respectively. Conclusion The anticancer activity of benzofuran [3,2-d] pyrimidine derivatives deserves further study.