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Synthesis and characterization of polyamide metallodendrimers and their anti-bacterial and anti-tumor activities

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Abstract

Pt(II) and Pd(II) complexes with aromatic amine terminated first generation (G1) and second generation (G2) polyamide dendrimers [PAD-(NH2) n ] (n = 6 for G1 and 12 for G2) were synthesized. All the synthesized dendrimers and metallodenrimers were characterized by elemental and spectral analysis. These novel dendrimers and their metallodendrimers (metal complexes of dendrimers) were screened for their anti-bacterial activity against Bacillus subtilis and Staphylococcus aureus (Gram positive) and Escherichia coli and Salmonella typhi (Gram negative) using agar disk diffusion method. The cytotoxicity assay of the dendrimers and metallodendrimers has been performed against MFC-7 cell lines using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Anti-bacterial evaluation indicates that the second generation dendrimer exhibit stronger biological activity against all the pathogenic bacterial strains in comparison to the first generation dendrimers. PdG2 exhibited lowest value of MIC 70 μg/ml against E. coli, while MIC value of PtG2 was 78 μg/ml. PdG2 and PtG2 show lowest anti-bacterial activity against S. typhi with 102 and 110 μg/ml (MIC value), respectively. In general, the metallodendrimers showed lower cytotoxicity than cisplatin (standard drug) and Pt(II) containing metallodendrimers were found to be more efficient in the induction of MFC-7 death than Pd(II) containing metallodendrimers.

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Acknowledgments

We would like to thank the College of Science Research Centre, King Saud University to support this work. Financial grant CHEM/2010/10.

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Authors and Affiliations

  1. Department of Chemistry, King Saud University, P.O. Box 2455, Riyadh, 11451, Kingdom of Saudi Arabia

    Tansir Ahamad & Saad M. Alshehri

  2. Department of Chemistry and Polymer Science, University of Stellenbosch, Private Bag X1, Matieland, 7602, South Africa

    S. F. Mapolie

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  1. Tansir Ahamad
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  2. S. F. Mapolie
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  3. Saad M. Alshehri
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Correspondence to Saad M. Alshehri.

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Ahamad, T., Mapolie, S.F. & Alshehri, S.M. Synthesis and characterization of polyamide metallodendrimers and their anti-bacterial and anti-tumor activities. Med Chem Res 21, 2023–2031 (2012). https://doi.org/10.1007/s00044-011-9715-0

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