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Evaluation of different PAMAM dendrimers as molecular vehicle of 1,2,4-triazine N-oxide derivative with potential antitumor activity

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Abstract

The interaction between a 1,2,4-triazine N-oxide derivative, that holds potential antitumor activity under hypoxic conditions, and diverse polyamidoamine (PAMAM) dendrimers were investigated with the purpose of select the most appropriate macromolecule to act as potential molecular carrier of this active compound. The results shows that dendrimers with amine terminal groups (PAMAM-AT G = 3) and dendrimers with carboxylate terminal groups (PAMAM-CT G2.5 and G4.5) produces triazine derivative hydrolysis, even in buffered medium, and are not suitable as carriers. In contrast, dendrimers with neutral end groups (PAMAM-OHT) shows stable association with the active compound, making this dendrimer a possible medium for triazine carriage.

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Acknowledgments

Financial support from the Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET-Argentina), Agencia Nacional de Promoción Científica y Tecnológica (FONCYT-Argentina), Secretaría de Ciencia y Técnica de la Universidad Nacional de Río Cuarto (SECYT-UNRC), is gratefully acknowledged.

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Authors and Affiliations

  1. Departamento de Física. Departamento de Química, Universidad Nacional de Río Cuarto, Agencia Postal 3, X5804BYA, Río Cuarto, Argentina

    Nahir Dib, Luciana Fernández, Edgardo Durantini, Luis Otero & Marisa Santo

  2. Grupo de Química Medicinal-Laboratorio de Química Orgánica. Facultad de Química. Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400, Montevideo, Uruguay

    Mercedes Gonzalez & Hugo Cerecetto

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  1. Nahir Dib
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  2. Luciana Fernández
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Correspondence to Luciana Fernández.

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Dib, N., Fernández, L., Gonzalez, M. et al. Evaluation of different PAMAM dendrimers as molecular vehicle of 1,2,4-triazine N-oxide derivative with potential antitumor activity. J Incl Phenom Macrocycl Chem 79, 65–73 (2014). https://doi.org/10.1007/s10847-013-0324-z

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  • DOI: https://doi.org/10.1007/s10847-013-0324-z

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