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Title 

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

Authors 

E VenkateswararaoV K SharmaJieun YunY KimS H Jung

Publisher 

Elsevier

Issue Date 

2014

Citation 

Bioorganic & Medicinal Chemistry, vol. 22, no. 13, pp. 3386-3392

Keywords 

Anti-proliferative activityChalconesInactivation of NF-κB

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.

ISSN 

0968-0896

Link 

http://dx.doi.org/10.1016/j.bmc.2014.04.045

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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