Synthesis and antitumor activities of 8-aminobenzofuran3, 2-d pyrimidine derivatives / 中国药学杂志

OBJECTIVE: To synthesize the derivatives of 8-amino benzofuran[3, 2-d] pyrimidine and study their anticancer activiies. METHODS: The target compounds were synthesized through a series of reactions, and their anticancer activities in vitro were evaluated 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 13C-NMR. Compounds 2, 3d and 5c had good inhibition effect against COLO205, MCF-7 and K562 cells. The inhibition rates of compound 5c against COLO205, MCF-7 and K562 cells were 99.58%, 78.75% and 98.68% respectively at 10-4 mol · L-1. CONCLUSION: The anticancer activity of benzofuran[3, 2-d] pyrimidine derivatives is worthy of further study.