Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 23, Pages 5797-5801Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.10.024
Keywords
Drug discovery; Anticancer; Structure-activity relationship; Benzoxaborole
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Funding
- National Science Foundation of China [81222042, 81573264, 21402118]
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In this study, we report the synthesis of a series of chalcone-benzoxaborole hybrid molecules and the evaluation of their anticancer activity. Their anticancer potency and toxicity were tested on three human cancer cell lines and two normal cell lines. The 4-fluoro compound 15 was found to be the most potent compound with an IC50 value of 1.4 mu M on SKOV3 cells. The 4-iodo compound 18 and 3-methyloxy-4-amino compound 47 showed good potency on SKOV3 cells while exhibiting low toxicity on normal cells. This work extended the application of benzoxaboroles to the field of anticancer research. (C) 2016 Elsevier Ltd. All rights reserved.
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