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Discovery of 1,4-pentadien-3-one derivatives containing quinoxaline scaffolds as potential apoptosis inducers.

Authors
  • Tang, Xu1
  • He, Jun1
  • Li, Qin1
  • Tang, Xuemei1
  • Chen, Mei1
  • Hao, Gefei1
  • Huai, Ziyou2
  • Huang, Yinjin2
  • Xue, Wei1
  • 1 State Key Laboratory Breeding Base of Green Pesticide & Agricultural Bioengineering, Center for Research & Development of Fine Chemicals, Guizhou University, Guiyang, Guizhou, 550025, China. , (China)
  • 2 School of Life Science, Bengbu Medical College, Anhui, Bengbu, 233030, China. , (China)
Type
Published Article
Journal
Future Medicinal Chemistry
Publisher
"Future Science, LTD"
Publication Date
Aug 01, 2020
Volume
12
Issue
16
Pages
1505–1519
Identifiers
DOI: 10.4155/fmc-2019-0371
PMID: 32772720
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

Aim: To synthesize novel antiproliferative agents. Results & methodology: A variety of 1,4-pentadien-3-one derivatives bearing quinoxaline scaffolds was designed and synthesized and their antiproliferative activities were evaluated. Notably, compounds N3 and N4 exhibited markedly greater antiproliferative activities against SMMC-7721 cells in vitro compared with the well-known antitumor drug gemcitabine. The mechanistic investigation showed that compounds N3 and N4 induced SMMC-7721 cell apoptosis by regulating the expression levels of apoptosis-related proteins. In addition, the molecular docking model further revealed that compound N3 could be a potential peroxisome proliferator-activated receptor inhibitor. Conclusion: These compounds might serve as bioactive fragments and lead compounds for developing more potent apoptosis inducers.

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