摘要 : A series of new tetrahydro[1]benzothieno[2,3-d]pyrimidines containing a 1,2,3-triazole fragment linked through an oxymethylene spacer have been synthesized by click reaction of 4-(prop-2-yn-1-yloxy)-5,6,7,8-tetrahydro[1]benzothien... 展开 A series of new tetrahydro[1]benzothieno[2,3-d]pyrimidines containing a 1,2,3-triazole fragment linked through an oxymethylene spacer have been synthesized by click reaction of 4-(prop-2-yn-1-yloxy)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidines with various aryl and alkyl azides in the presence of copper sulfate and sodium ascorbate as a catalyst. The structures of the synthesized compounds were characterized by various spectroscopic techniques (H-1 and C-13 NMR, FT-IR, and mass spectrometry), and their in vitro anticancer activity against NCI-60 human tumor cell lines was evaluated. Among the compounds tested, N-(pyridine-3-yl)-acetamide derivative exhibited significant activity against several cancer cell lines, including SF-539 (CNS cancer), HCT-116 (colon cancer), OVCAR-8 (ovarian cancer), PC-3 (prostate cancer), and CCRF-CEM (leukemia). 收起