Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 22, Issue 13, Pages 3386-3392Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.04.045
Keywords
Chalcones; Inactivation of NF-kappa B; Anti-proliferative activity
Funding
- Priority Research Centers Program through the National Research Foundation of Korea (NRF) - Ministry of Education, Science and Technology [2009-0093815]
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To investigate the anti-proliferative effect of NF-kappa B inhibitor, a series of analogs of (E)-1-(2-hydroxy-6-(isopentyloxy)phenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one (5a) were prepared and evaluated for their NE-kappa B inhibition and anti-proliferative activity against various human cancer cell lines. Compounds (E)-1-(2-(3,3-dimethylbutoxy)-6-hydroxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one (5e) and (E)-4-(3-(2-(3,3-dimethylbutoxy)-6-hydroxyphenyl)-3-oxoprop-1-enyl)benzenesulfonamide (5p) showed good NF-kappa B inhibition as well as potent anti-proliferative activity. SAR studies showed that all the compounds with potent or moderate NF-kappa B inhibition displayed good anti-proliferative activity. All the analogs (5b-r) maintained a good correlation between their NE-kappa B inhibition and anti-proliferative activity though the extent is not directly proportional to each other. (C) 2014 Elsevier Ltd. All rights reserved.
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