期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 11, 页码 2023-2028出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.04.060
关键词
2-Alkoxy-5-hydroxy-1,4-naphthoquinone; Anticancer activity; Chemical reactivity
资金
- Priority Research Centers Program through the National Research Foundation of Korea (NRF) - Ministry of Education, Science and Technology [2009-0093815]
To establish the structure-activity relationship of 5-hydroxy-1,4-naphthoquinones toward anticancer activity, a series of its derivatives were prepared and tested for the activity (IC50 in mu M) against three cell lines; colo205 (colon adenocarcinoma), T47D (breast ductal carcinoma) and K562 (chronic myelogenous leukemia). Among them 2 (IC50: 2.3; 2.0; 1.4 mu M), 6 (IC50: 1.9; 2.2; 1.3 mu M), 9 (IC50: 0.7; 1.7; 0.9 mu M) and 10 (IC50:1.7; 1.0; 1.2 mu M) showed moderate to excellent activity. Our perception toward the DNA substitution of alkoxy groups at the C2 position of these naphthoquinones for the anticancer activity led us to investigate their reactivity of substitution toward dimethylamine as a nucleophile. The ease of the substitution of alkoxy groups at the C2 position with dimethylamine is strongly accelerated by hydroxyl group at C5 position and is well correlated with the found anticancer activity results. (C) 2018 Elsevier Ltd. All rights reserved.
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