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Design and synthesis of pregnenolone/2-cyanoacryloyl conjugates with dual NF-κB inhibitory and anti-proliferative activities.

Authors
  • Song, Jia-Li1
  • Zhang, Juan2
  • Liu, Chang-Liang3
  • Liu, Chao4
  • Zhu, Kong-Kai1
  • Yang, Fei-Fei1
  • Liu, Xi-Gong1
  • Figueiró Longo, João Paulo2
  • Alexandre Muehlmann, Luis2
  • Azevedo, Ricardo Bentes5
  • Zhang, Yu-Ying6
  • Guo, Yue-Wei7
  • Jiang, Cheng-Shi8
  • Zhang, Hua9
  • 1 School of Biological Science and Technology, University of Jinan, Jinan 250022, China. , (China)
  • 2 Faculty of Ceilandia, University of Brasilia, Brasilia 72220275, Brazil; Institute of Biological Sciences, University of Brasília, Brasília 70910900, Brazil. , (Brazil)
  • 3 Department of Neurobiology, Harvard Medical School, Boston, MA 02115, USA.
  • 4 Institute of Agro-Food Science and Technology, Shandong Academy of Agricultural Sciences, Jinan 250100, China. , (China)
  • 5 Institute of Biological Sciences, University of Brasília, Brasília 70910900, Brazil. , (Brazil)
  • 6 School of Biological Science and Technology, University of Jinan, Jinan 250022, China. Electronic address: [email protected] , (China)
  • 7 Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. , (China)
  • 8 School of Biological Science and Technology, University of Jinan, Jinan 250022, China. Electronic address: [email protected] , (China)
  • 9 School of Biological Science and Technology, University of Jinan, Jinan 250022, China. Electronic address: [email protected] , (China)
Type
Published Article
Journal
Bioorganic & medicinal chemistry letters
Publication Date
Oct 15, 2017
Volume
27
Issue
20
Pages
4682–4686
Identifiers
DOI: 10.1016/j.bmcl.2017.09.013
PMID: 28919340
Source
Medline
Keywords
License
Unknown

Abstract

Twenty-five novel pregnenolone/2-cyanoacryloyl conjugates (6-30) were designed and prepared, with the aim of developing novel anticancer drugs with dual NF-κB inhibitory and anti-proliferative activities. Compounds 22 and 27-30 showed inhibition against TNF-α-induced NF-κB activation in luciferase assay, which was confirmed by Western blotting. Among them, compound 30 showed potent NF-κB inhibitory activity (IC50=2.5μM) and anti-proliferative against MCF-7, A549, H157, and HL-60 cell lines (IC50=6.5-36.2μM). The present study indicated that pregnenolone/2-cyanoacryloyl conjugate I can server asa novel scaffold for developing NF-κB inhibitors and anti-proliferative agents in cancer chemotherapy.

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