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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Original multivalent copper(II)-conjugated phosphorus dendrimers and corresponding mononuclear copper(II) complexes with antitumoral activities
Molecular Pharmaceutics, Volume 10, No. 4, Year 2013
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Description
Novel multivalent copper(II)-conjugated phosphorus dendrimers and their corresponding mononuclear copper(II) complexes were synthesized, characterized, and screened for antiproliferative activity against human cancer cell lines. Selected copper ligands were grafted on the surface of phosphorus dendrimers of generation Gn (n = 1 to 3): N-(pyridin-2-ylmethylene)ethanamine for dendrimers 1Gn, N-(di(pyridin-2-yl)methylene)ethanamine for dendrimers 2Gn, and 2-(2-methylenehydrazinyl)pyridine for dendrimers 3Gn. The results indicated that the most potent derivatives are 1Gn and 1Gn-Cu versus 2Gn, 2Gn-Cu, and 3Gn, 3Gn-Cu. A direct relationship between the growth inhibitory effect and the number of terminal moieties or the amount of copper complexed to the dendrimer was observed in copper-complexed 1 series and noncomplexed 1 series. These data clearly suggested that cytotoxicity increased with the number of terminal moieties available and was boosted by the presence of complexed Cu atoms. Importantly, no cytotoxic effect was observed with CuCl2 at the same concentrations. Finally, 1G3 and 1G 3-Cu have been selected for antiproliferative studies against a panel of tumor cell lines: 1G3 and 1G3-Cu demonstrated potent antiproliferative activities with IC50 values ranging 0.3-1.6 μM. Interestingly, the complexation of the terminal ligands of 1G3 dendrimers by copper(II) metal strongly increased the IC50 values in noncancer cells lines referred to as "safety" cell lines. © 2013 American Chemical Society.
Authors & Co-Authors
El Brahmi, Nabil
Morocco, Agdal Rabat
Innovation and Research Mascir Foundation
Morocco, Rabat
Faculté Des Sciences Rabat
France, Toulouse
Lcc Laboratoire de Chimie de Coordination
El Kazzouli, Saïd
Morocco, Agdal Rabat
Innovation and Research Mascir Foundation
Mignani, Serge M.
France, Paris
Université Paris Cité
Essassi, El Mokhtar
Morocco, Rabat
Faculté Des Sciences Rabat
Aubert, Geneviève
France, Gif-sur-yvette
Institut de Chimie Des Substances Naturelles
Laurent, Régis
France, Toulouse
Lcc Laboratoire de Chimie de Coordination
Caminade, Anne Marie
France, Toulouse
Lcc Laboratoire de Chimie de Coordination
Bousmina, Mostapha M.
Morocco, Rabat
Al Akhawayn University, Hassan Ii Academy of Sciences and Technology
Morocco, Fez
Université Euro-méditerranéenne de Fès
Cresteil, Thierry
France, Gif-sur-yvette
Institut de Chimie Des Substances Naturelles
Majoral, Jean Pierre
France, Toulouse
Lcc Laboratoire de Chimie de Coordination
Statistics
Citations: 83
Authors: 10
Affiliations: 7
Identifiers
Doi:
10.1021/mp4000184
ISSN:
15438384
e-ISSN:
15438392
Research Areas
Cancer