Anti-proliferative effect of chalcone derivatives through inactivation of NF-κB in human cancer cells

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Title
Anti-proliferative effect of chalcone derivatives through inactivation of NF-κB in human cancer cells
Author(s)
E Venkateswararao; V K Sharma; Jieun Yun; Y Kim; S H Jung
Bibliographic Citation
Bioorganic & Medicinal Chemistry, vol. 22, no. 13, pp. 3386-3392
Publication Year
2014
Abstract
To investigate the anti-proliferative effect of NF-κB 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 NF-κB 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-κB inhibition as well as potent anti-proliferative activity. SAR studies showed that all the compounds with potent or moderate NF-κB inhibition displayed good anti-proliferative activity. All the analogs (5b-r) maintained a good correlation between their NF-κB inhibition and anti-proliferative activity though the extent is not directly proportional to each other.
Keyword
Anti-proliferative activityChalconesInactivation of NF-κB
ISSN
0968-0896
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmc.2014.04.045
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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