Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 21, Pages 6993-6999Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.09.037
Keywords
(5Z)-7-Oxozeaenol; TAK1; Selectfluor (R); Covalent docking; Resorcylic acid lactone
Funding
- National Cancer Institute/National Institutes of Health [P01 CA125066]
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(5Z)-7-Oxozeanol and related analogues were isolated and screened to explore their activity as TAK1 inhibitors. Seven analogues were synthesized and more than a score of natural products isolated that examined the role that different areas of the molecule contribute to TAK1 inhibition. A novel nonaromatic difluoro-derivative was synthesized that had similar potency compared to the lead. This is the first example of a nonaromatic compound in this class to have TAK1 inhibition. Covalent docking for the isolated and synthesized analogues was carried out and found a strong correlation between the observed activities and the calculated binding. (C) 2015 Elsevier Ltd. All rights reserved.
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