当前位置: X-MOL 学术RSC Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Cu(II) immobilized on Fe3O4@APTMS-DFX nanoparticles: an efficient catalyst for the synthesis of 5-substituted 1H-tetrazoles with cytotoxic activity
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-09-15 00:00:00 , DOI: 10.1039/c7md00302a
Faezeh Taghavi 1, 2, 3, 4, 5 , Mostafa Gholizadeh 1, 2, 3, 4, 5 , Amir Sh. Saljooghi 1, 2, 3, 4, 5 , Mohammad Ramezani 4, 5, 6, 7, 8
Affiliation  

Cu(II) immobilized on deferasirox loaded amine functionalized magnetic nanoparticles (Cu(II)/Fe3O4@APTMS-DFX) as a novel magnetically recyclable heterogeneous catalyst is able to catalyze the [3 + 2] cycloaddition reactions of various organic nitriles with sodium azide. Using this method, a series of 5-substituted-1H-tetrazoles under mild conditions in DMSO were prepared. The reaction involves mild reaction conditions with efficient transformation capability. The developed catalyst could be easily separated by applying an external magnetic field. Furthermore, it could be recycled for 5 runs with negligible leaching of copper from the surface of the catalyst. The catalyst was characterized by various techniques such as FT-IR, TGA, VSM, SEM-EDX, and ICP-OES. Several derivatives of 1H-tetrazoles were prepared using this catalyst, and their structures were confirmed using different techniques. Then, the synthesized anthraquinones were evaluated for their cytotoxicity against several cell lines including MCF-7, MAD-MD-231, HT-29, HeLa, neuro-2a and L-929. The results obtained from the MTT assay revealed that the 6 derivatives exhibited a high level of cytotoxicity. In order to determine the cytotoxicity mechanism, 2 derivatives with the highest cytotoxic activity were selected, and an apoptosis assay was carried out by flow cytometry, which supported that apoptosis is the major mechanism.

中文翻译:

固定在Fe 3 O 4 @ APTMS-DFX纳米颗粒上的Cu(II):一种合成具有细胞毒活性的5取代1 H-四唑的有效催化剂

铜(II固定在地拉罗司装载胺)官能化的磁性纳米颗粒(铜(II)/ Fe的3 ö 4 @ APTMS-DFX)作为一种新的磁性可回收的非均相催化剂是能够催化各种有机腈的[3 + 2]环加成反应与叠氮化钠。使用这种方法,一系列5取代的1 H在温和条件下的DMSO中制备了四唑。该反应涉及具有有效转化能力的温和反应条件。通过施加外部磁场可以很容易地分离出显影的催化剂。此外,它可以循环使用5次,而从催化剂表面浸出的铜几乎可以忽略不计。通过多种技术对催化剂进行了表征,例如FT-IR,TGA,VSM,SEM-EDX和ICP-OES。1 H的几种导数用该催化剂制备-四唑,并用不同的技术证实它们的结构。然后,评估了合成的蒽醌对几种细胞系的细胞毒性,所述细胞系包括MCF-7,MAD-MD-231,HT-29,HeLa,neuro-2a和L-929。从MTT分析获得的结果表明6种衍生物表现出高水平的细胞毒性。为了确定细胞毒性机理,选择了两种具有最高细胞毒性活性的衍生物,并通过流式细胞术进行了凋亡分析,这证明了凋亡是主要的机制。
更新日期:2017-10-18
down
wechat
bug