N, N ' -双([1,2,4]三唑[4,3-b][1,2,4,5]四氮-6-基)烷基胺衍生物的合成、生物学评价及分子对接

Journal of Chemical Research-s Pub Date : 2022-09-01 DOI:10.1177/17475198221123516

Zhonglu Ke, Tianyun Pei, Zhenzhen Yang, Xuanhe Zhang, Feng Xu, Zihang Xu, Jixiang Ding

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引用次数: 0

摘要

设计、合成了一系列N, N′-双([1,2,4]三唑[4,3-b][1,2,4,5]四嗪-6-基)烷基胺衍生物，并对其对三种肿瘤细胞系的抑制活性和体外c-Met激酶活性进行了评价。这些化合物通过1H NMR, 13C NMR, MS, IR和元素分析得到了完整的表征。抗肿瘤实验表明，部分化合物对A549、Bewo和MCF-7癌细胞具有明显的抑制作用。其中，4a的IC50值显示对A549 (1.21 μM)、Bewo (0.68 μM)和MCF-7 (3.74 μM)细胞株的抗肿瘤活性优于阳性剂顺铂(A549、Bewo和MCF-7分别为9.97 μM、10.46 μM和15.03 μM)。

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Synthesis, biological evaluation and molecular docking of N, N’-bis([1,2,4]triazole[4,3-b][1,2,4,5]tetrazine-6-yl)alkylamine derivatives as potent c-Met antagonists

A series of N, N’-bis([1,2,4]triazole[4,3-b][1,2,4,5]tetrazine-6-yl)alkylamine derivatives is designed, synthesized and evaluated for their inhibition activities against three tumor cell lines and c-Met kinase activity in vitro. These compounds are fully characterized by 1H NMR, 13C NMR, MS, IR and elemental analysis. Antitumor experiments indicate that some of these compounds exhibit significant inhibition activities against A549, Bewo and MCF-7 cancer cell lines. Among them, the IC50 values of 4a indicate better antitumor activities against the A549 (1.21 μM), Bewo (0.68 μM) and MCF-7 (3.74 μM) cell lines than the positive agent cisplatin (9.97 μM for A549, 10.46 μM for Bewo, and 15.03 μM for MCF-7), respectively.

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来源期刊

Journal of Chemical Research-s 化学科学, 有机化学, 有机合成

自引率

0.00%

发文量

审稿时长

1 months

期刊介绍： The Journal of Chemical Research is a peer reviewed journal that publishes full-length review and research papers in all branches of experimental chemistry. The journal fills a niche by also publishing short papers, a format which favours particular types of work, e.g. the scope of new reagents or methodology, and the elucidation of the structure of novel compounds. Though welcome, short papers should not result in fragmentation of publication, they should describe a completed piece of work. The Journal is not intended as a vehicle for preliminary publications. The work must meet all the normal criteria for acceptance as regards scientific standards. Papers that contain extensive biological results or material relating to other areas of science may be diverted to more appropriate specialist journals. Areas of coverage include: Organic Chemistry; Inorganic Chemistry; Materials Chemistry; Crystallography; Computational Chemistry.