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Design, synthesis and in vitro biological evaluation of novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing a thiosemicarbazide moiety
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2018-01-17 , DOI: 10.1016/j.ejmech.2018.01.031
Peng-Fei Geng , Xue-Qi Liu , Tao-Qian Zhao , Cong-Cong Wang , Zhong-Hua Li , Ji Zhang , Hao-Ming Wei , Biao Hu , Li-Ying Ma , Hong-Min Liu

A series of hybrid molecules containing [1,2,3]triazolo[4,5-d]pyrimidine and thiosemicarbazide moieties were designed, synthesized and evaluated for their antiproliferative activities against MGC-803, NCI-H1650 and PC-3 human cancer cells. Some of the synthesized compounds showed moderate to good activity against three selected cancer cell lines. Among these compounds, compound 29 displayed the most potent antiproliferative activity as well as good selectivity between cancer cells and normal cells. Further mechanism studies revealed that compound 29 could obviously inhibit the colony formation and migration of MGC-803 as well as induced apoptosis.



中文翻译:

新型[1,2,3]三唑并[4,5-d]嘧啶衍生物的设计,合成及体外生物学评价

设计,合成和评估了一系列含有[1,2,3]三唑并[4,5-d]嘧啶和硫代氨基脲部分的杂合分子,它们对MGC-803,NCI-H1650和PC-3人癌细胞的抗增殖活性。一些合成的化合物对三种选定的癌细胞系显示出中等至良好的活性。在这些化合物中,化合物29在癌细胞与正常细胞之间显示出最有效的抗增殖活性以及良好的选择性。进一步的机理研究表明,化合物29可以明显抑制MGC-803的菌落形成和迁移以及诱导的细胞凋亡。

更新日期:2018-01-17
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