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Design, synthesis, and antitumor evaluation of novel anthraquinone derivatives

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Abstract

N-alkylated and O-alkylated anthraquinone derivatives with structures analogous to mitoxantrone were synthesized, characterized, and evaluated for their cytotoxic properties against three tumor cell lines (Human Breast Adenocarcinoma MCF-7, Human Cervical Adenocarcinoma HeLa, and Human Glioblastoma M059J) and a normal cell line (human lung fibroblasts GM-07492A). A structure-activity relationship study was carried out to verify the influence of lipophilic chain size on the biological activity of these compounds. The results indicated promising candidates for antineoplastic agents for the cancers evaluated, since these compounds showed significant selectivity and high cytotoxic potential for cancer cells, rather than mitoxantrone, the compound of which is already used in anticancer therapy.

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Acknowledgements

This work was supported by grants from FAPEMIG, CNPq, CAPES, Rede Mineira de Química, and UFJF.

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Authors and Affiliations

  1. Departamento de Química, Universidade Federal de Juiz de Fora, Juiz de Fora, MG, 36036-330, Brazil

    Larissa A. Oliveira, Nerilson M. Lima & Mauro V. Almeida

  2. Universidade de Franca, Franca, SP, 14404600, Brazil

    Heloiza D. Nicolella, Ricardo A. Furtado & Denise C. Tavares

  3. Departamento de Ciências Exatas e da Terra, Universidade do Estado de Minas Gerais, Frutal, MG, 38200000, Brazil

    Taís A. Corrêa

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  1. Larissa A. Oliveira
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  2. Heloiza D. Nicolella
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  3. Ricardo A. Furtado
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  4. Nerilson M. Lima
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  5. Denise C. Tavares
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  6. Taís A. Corrêa
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  7. Mauro V. Almeida
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Correspondence to Mauro V. Almeida.

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Oliveira, L.A., Nicolella, H.D., Furtado, R.A. et al. Design, synthesis, and antitumor evaluation of novel anthraquinone derivatives. Med Chem Res 29, 1611–1620 (2020). https://doi.org/10.1007/s00044-020-02587-4

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  • DOI: https://doi.org/10.1007/s00044-020-02587-4

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