2. Academic Validation
  3. Anti-proliferative effect of chalcone derivatives through inactivation of NF-κB in human cancer cells

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

  • Bioorg Med Chem. 2014 Jul 1;22(13):3386-92. doi: 10.1016/j.bmc.2014.04.045.
Eeda Venkateswararao 1,  Vinay K Sharma 1,  Jieun Yun 2,  Youngsoo Kim 3,  Sang-Hun Jung 4
Affiliations

Affiliations

  • 1 College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, South Korea.
  • 2 Bioevaluation Center, Korea Research Institute of Bioscience and Biotechnology, Cheongwon 363-883, South Korea.
  • 3 College of Pharmacy, Chungbuk National University, Cheongju 361-763, South Korea.
  • 4 College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, South Korea. Electronic address: jungshh@cnu.ac.kr.
PMID: 24835787 DOI: 10.1016/j.bmc.2014.04.045
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.

Keywords

Anti-proliferative activity; Chalcones; Inactivation of NF-κB.

Figures