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Synthesis, characterisation and cytotoxic activity evaluation of new metal-salen complexes based on the 1,2-bicyclo[2.2.2]octane bridge
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2020-12-11 , DOI: 10.1016/j.tetlet.2020.152706
Pierre Milbeo , François Quintin , Laure Moulat , Claude Didierjean , Jean Martinez , Xavier Bantreil , Monique Calmès , Frédéric Lamaty

(R)-1,2-Diaminobicyclo[2.2.2]octane was used as a starting material for the preparation, in solution or in a ball mill, of a salen ligand. Five metal salen complexes were prepared in high yield and their cytotoxic activities were evaluated against the Human Colon cancer HCT116 cell lines. The original manganese salen complex displayed the highest activity with a potency 16 fold higher than that of cisplatin, demonstrating the benefit of the bridging backbone compared to other salen systems. An alternative preparation route for this complex by mechanochemistry was also performed.



中文翻译:

基于1,2-双环[2.2.2]辛烷桥的新型金属-沙仑配合物的合成,表征和细胞毒活性评估

R)-1,2-二氨基双环[2.2.2]辛烷用作在溶液中或在球磨机中制备salen配体的原料。高产率地制备了五种金属塞伦复合物,并评估了它们对人结肠癌HCT116细胞系的细胞毒性活性。原始的锰锡兰复合物显示出最高的活性,效力比顺铂高16倍,这证明了与其他锡兰体系相比,桥接主链的益处。还通过机械化学方法对该复合物进行了另一种制备方法。

更新日期:2021-01-07
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