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Impact of the carbon chain length of novel platinum complexes derived from N-alkyl-propanediamines on their cytotoxic activity and cellular uptake |
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| Authors: | Silva Heveline Valério Barra Carolina França da Costa Cristiane de Almeida Mauro Vieira César Eloi Teixeira Silveira Josianne N Garnier-Suillerot Arlette Silva de Paula Flávia Cristina Pereira-Maia Elene Cristina Fontes Ana Paula Soares |
| Institution: | a Departamento de Química, Universidade Federal de Juiz de Fora, 36036-900 Juiz de Fora-MG, Brazil b Colégio de Aplicação João XXIII, Juiz de Fora-MG, Brazil c Departamento de Análises Clínicas e Toxicológicas - Faculdade de Farmácia, Universidade Federal de Minas Gerais, 31.270-901 Belo Horizonte-MG, Brazil d Laboratoire de Physicochimie Biomoléculaire et cellulaire (ESA 7033), Université Paris Nord, Bobigny, France e Departamento de Química, Universidade Federal de Minas Gerais, Belo Horizonte-MG, Brazil |
| Abstract: | This work describes the synthesis and characterization of four new ligands derived from 1,3-propanediamine in addition to the preparation and characterization of their respective platinum(II) complexes by reaction with K2PtCl4. These ligands were obtained by the reaction of the corresponding alkyl mesylate with 1,3-propanediamine. We have prepared compounds having different carbon chains lengths in an attempt to correlate this factor, which influences the lipophilicity of the compounds, with cytotoxic activity. Octanol/water partition coefficients, the effect of the four complexes on the growth of two tumoral cell lines, and their cellular uptake were investigated. Increasing lipophilicity enhances the rate of cellular uptake and, consequently, the cytotoxic activity. |
| Keywords: | Amines Platinum Antitumor agents Cellular uptake Lipophilicity |
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