Journal
MOLECULAR PHARMACEUTICS
Volume 14, Issue 11, Pages 4087-4097Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.molpharmaceut.7b00771
Keywords
dendrimers; gold complexes; copper complexes; antitumoral agents; antimicrobial agents
Funding
- CNRS (France)
- University of Lodz (Poland)
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Original metallophosphorus dendrimers (generation 3, 48 terminal groups) have been prepared via the complexation of phosphorus dendrimers bearing iminopyridino end groups with Au(III) or with both Au(III) and Cu(II). The complexation of the dendrimer with Au(III), leading to 1G3-[Au-48][AuCl4](48), strongly increased the antiproliferative activities against both KB and HL-60 tumoral cell lines, showing IC(50)s in the low nanomolar range. It can be noticed also that this gold conjugated phosphorus dendrimer displayed low activity on the quiescent cell line EPC versus its potent antiproliferative activity against actively dividing cells. In order to evaluate the potential synergistic effect between Au(III) and Cu(II) and the influence of the number of Au(III) moieties on the surface of dendrimer against the proliferative activities, nine other original dendrimers with several surface modifications have been prepared. Whatever the number of Au(III) moieties introduced on the surface of dendrimers, all the dendrimers prepared displayed similar potency (nanomolar range) to 1G3-[Au-48][AuCl4](48) against KB and HL60. In marked contrast synergistic effects on the antimicrobial activity of some of these phosphorus dendrimers are observed when both Au(III) and Cu(II) are present on the dendritic structure.
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