新型[1,2,4]三唑并[4,3-a]嘧啶的三组分一锅法合成及抗增殖活性。
Three Component One-Pot Synthesis and Antiproliferative Activity of New [1,2,4]Triazolo[4,3-]pyrimidines.
机构信息
Laboratory of Applied Chemistry: Heterocycles, Lipids, and Polymers, Faculty of Sciences of Sfax, University of Sfax, Sfax 3000, Tunisia.
Laboratory of Molecular and Cellular Screening Processes, Centre of Biotechnology of Sfax, Sfax 3018, Tunisia.
出版信息
Molecules. 2023 May 5;28(9):3917. doi: 10.3390/molecules28093917.
A series of new [1,2,4]triazolo[4,3-a]pyrimidine derivatives was prepared using a one-pot three-component synthesis from 5-amino-1-phenyl-1-1,2,4-triazoles, aromatic aldehydes and ethyl acetoacetate. The compound structures were confirmed by IR, H-NMR, C-NMR, HRMS and X-ray analyses. The biological activity of these compounds as antitumor agents was evaluated. Their antitumor activities against cancer cell lines (MDA-MB-231 and MCF-7) were tested by the MTT in vitro method. Among them, compounds and displayed the best antitumor activity with IC values of 17.83 μM and 19.73 μM against MDA-MB-231 and MCF-7 cell lines, respectively, compared to the Cisplatin reference.
一系列新型[1,2,4]三唑并[4,3-a]嘧啶衍生物采用一锅法三组分合成法，由 5-氨基-1-苯基-1-1,2,4-三唑、芳香醛和乙酰乙酸乙酯制备。通过 IR、H-NMR、C-NMR、HRMS 和 X 射线分析确认了化合物结构。评估了这些化合物作为抗肿瘤剂的生物活性。通过 MTT 体外法测试了它们对癌细胞系（MDA-MB-231 和 MCF-7）的抗肿瘤活性。其中，化合物 和 表现出最好的抗肿瘤活性，对 MDA-MB-231 和 MCF-7 细胞系的 IC 值分别为 17.83 μM 和 19.73 μM，优于顺铂对照。
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