4.4 Article

Synthesis, characterisation and cytotoxic activity evaluation of new metal-salen complexes based on the 1,2-bicyclo[2.2.2]octane bridge

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TETRAHEDRON LETTERS
卷 63, 期 -, 页码 -

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2020.152706

关键词

Salen metal complex; Manganese; Mechanochemistry; Cytotoxicity; HCT116

资金

  1. Universite de Montpellier, Centre Nationale de la Recherche Scientifique (CNRS)
  2. Agence Nationale de la Recherche [ANR-16-CE07-0009-01]
  3. Agence Nationale de la Recherche (ANR) [ANR-16-CE07-0009] Funding Source: Agence Nationale de la Recherche (ANR)

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(R)-1,2-Diaminobicyclo[2.2.2]octane was used to prepare a salen ligand, and five metal salen complexes were synthesized with high yield. The original manganese salen complex showed the highest cytotoxic activity, being 16 times more potent than cisplatin, highlighting the advantage of the bridging backbone. An alternative mechanochemical method for preparing this complex was also explored.
(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. (C) 2020 Elsevier Ltd. All rights reserved.

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