新型含硫代缩氨基脲部分的[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。
Design, synthesis and in vitro biological evaluation of novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives containing a thiosemicarbazide moiety.
机构信息
Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, PR China.
Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Technology of Drug Preparation (Zhengzhou University), Ministry of Education of China, Key Laboratory of Henan Province for Drug Quality and Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, PR China.
出版信息
Eur J Med Chem. 2018 Feb 25;146:147-156. doi: 10.1016/j.ejmech.2018.01.031. Epub 2018 Jan 17.
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.
设计、合成了一系列含有[1,2,3]三唑并[4,5-d]嘧啶和缩硫脲片段的杂化分子，并评价了它们对 MGC-803、NCI-H1650 和 PC-3 人癌细胞的增殖抑制活性。一些合成的化合物对三种选定的癌细胞系表现出中等至良好的活性。在这些化合物中，化合物 29 表现出最强的增殖抑制活性以及癌细胞和正常细胞之间良好的选择性。进一步的机制研究表明，化合物 29 能明显抑制 MGC-803 的集落形成和迁移，并诱导细胞凋亡。
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