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Synthesis and biological evaluation of novel 2,3-dihydrochromeno[3,4-d]imidazol-4(1H)-one derivatives as potent anticancer cell proliferation and migration agents.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2016 Feb 5 , DOI: 10.1016/j.ejmech.2016.01.035 Xuan Han , Jiang Luo , Feng Wu , XueYan Hou , Guoyi Yan , Meng Zhou , Mengqi Zhang , Chunlan Pu , Rui Li
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2016 Feb 5 , DOI: 10.1016/j.ejmech.2016.01.035 Xuan Han , Jiang Luo , Feng Wu , XueYan Hou , Guoyi Yan , Meng Zhou , Mengqi Zhang , Chunlan Pu , Rui Li
In this study, a series of novel molecules containing chromeno [3,4-d] imidazol-4(1H)-one was synthesized and their biological activities were evaluated. Among them, compound 35 showed a dramatic anticancer activity against HCT116 and MCF-7, and the flow cytometry assays demonstrated that it could arrest G0/G1 cell-cycle and induce apoptosis of SW620 cells in a dose-dependent manner. Besides, it also blocked MCF-7 cancer cell migration. Moreover, it inhibited tumor growth in HCT116 subcutaneously implanted xenografted mice. Taken together, compound 35 may be a promising candidate for anti-cancer agent as well as metastatic one.
中文翻译:
新型2,3-二氢色素[3,4-d]咪唑-4(1H)-one衍生物的合成和生物学评估,该衍生物为有效的抗癌细胞增殖和迁移剂。
在这项研究中,合成了一系列的新分子,其中包含chromeno [3,4-d] imidazol-4(1H)-one,并对其生物学活性进行了评估。其中,化合物35对HCT116和MCF-7表现出显着的抗癌活性,流式细胞仪检测表明它可以阻滞G0 / G1细胞周期并诱导SW620细胞凋亡,并呈剂量依赖性。此外,它还阻止了MCF-7癌细胞的迁移。此外,它抑制了HCT116皮下植入异种移植小鼠的肿瘤生长。两者合计,化合物35可能是抗癌药以及转移性药物的有希望的候选者。
更新日期:2017-01-31
中文翻译:
新型2,3-二氢色素[3,4-d]咪唑-4(1H)-one衍生物的合成和生物学评估,该衍生物为有效的抗癌细胞增殖和迁移剂。
在这项研究中,合成了一系列的新分子,其中包含chromeno [3,4-d] imidazol-4(1H)-one,并对其生物学活性进行了评估。其中,化合物35对HCT116和MCF-7表现出显着的抗癌活性,流式细胞仪检测表明它可以阻滞G0 / G1细胞周期并诱导SW620细胞凋亡,并呈剂量依赖性。此外,它还阻止了MCF-7癌细胞的迁移。此外,它抑制了HCT116皮下植入异种移植小鼠的肿瘤生长。两者合计,化合物35可能是抗癌药以及转移性药物的有希望的候选者。