Identification of ortho-naphthoquinones as anti-AML agents by highly efficient oxidation of phenols |
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| Institution: | 1. Department of Urology, The Third Xiangya Hospital of Central South University, Central South University, Changsha 410000, China;2. Department of Urology, Xiangya Hospital of Central South University, Central South University, Changsha 410000, China;3. Department of Urology, The Fifth Affiliated Hospital of Sun Yat-sen University, Sun Yat-sen University, Zhuhai 519000, China;1. Department of Chemistry, Faculty of Sciences, University of Chile, Las Palmeras 3425, 780003 Ñuñoa, Santiago, Chile;2. Department of Chemistry, Faculty of Basic Sciences, Metropolitan Educational Sciences University, Av. José Pedro Alessandri 774, 7760197 Ñuñoa, Santiago, Chile;3. Clinical and Molecular Pharmacology Program, Institute of Biomedical Sciences (ICBM), Faculty of Medicine, University of Chile, Av. Independencia 1027, Santiago 8380453, Chile;4. Cell Culture Laboratory, Faculty of Health Sciences, University of Talca, 824000, Av. Lircay, Talca, Chile;5. Institute of Chemistry and Biochemistry, Faculty of Sciences, University of Valparaiso, 2360102, Av. Gran Bretaña 1111, Playa Ancha, Valparaiso, Casilla 5030, Chile;6. Centro de Investigación Farmacopea Chilena (CIFAR), University of Valparaíso, 2360134, Santa Marta 183, Valparaíso, Chile;7. Department of Organic Chemistry and Physical Chemistry, Faculty of Chemical and Pharmaceutical Sciences, University of Chile, Santos Dumont 964, 8330015 Santiago, Chile |
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| Abstract: | A straightforward method for synthesizing ortho-naphthoquinones was identified using an easily available cobalt–Schiff base complex. Efficient oxidation of phenols to ortho-naphthoquinones was useful in obtaining compounds with potent biological activity for the treatment of acute myeloid leukemia (AML). Among these compounds, the compound 4h effectively inhibited the proliferation of different AML cell lines in vitro. Further in vivo antitumor studies indicated that 4h at 40 mg/kg/d led to tumor regression in led to tumor regression in an MV4-11 xenograft model without evident toxicity. The cobalt-Schiff base complex was found to be an efficient catalyst in the transformation of phenols to ortho-quinones, and the compound 4h represents a potential scaffold to optimize the production of a treatment for AML. |
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