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Bioorg Chem. 2019 May;86:97-102. doi: 10.1016/j.bioorg.2019.01.025. Epub 2019 Jan 18.

Identification of ortho-naphthoquinones as anti-AML agents by highly efficient oxidation of phenols.

Author information

1
Department of Pharmaceutical Engineering, China Pharmaceutical University, Nanjing 210009, China.
2
Department of Food Quality and Safety, School of Engineering, China Pharmaceutical University, Nanjing 211816, China.
3
College of Biotechnology and Pharmaceutical Engineering, Nanjing Tech University, Nanjing 211816, China. Electronic address: gaozhen@njtech.edu.cn.
4
Department of Pharmaceutical Engineering, China Pharmaceutical University, Nanjing 210009, China. Electronic address: ccj33@163.com.

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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