Synthesis of selenophene-based chalcone analogs and assessment of their biological activity as anticancer agents

Ya Chen Chen, Cai Wei Li, Jih Jung Chen*, Tzenge Lien Shih*

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

2 Scopus citations

Abstract

Selenium is an essential micronutrient that is beneficial to human health. Selenium-containing drugs have been developed as antioxidants, anti-inflammatory, and anticancer agents. However, the synthesis of selenium-containing chalcones has not been fully explored. Therefore, we report the synthesis of novel selenophene-based chalcone analogs and reveal their biological activities as anticancer agents. Among the seven synthesized molecules, compounds 6, 8, and 10 exhibited anticancer activity with IC50 values of 19.98 ± 3.38, 38.23 ± 3.30, and 46.95 ± 5.68 μM, respectively, against human colorectal adenocarcinoma (HT-29) cells. Clonogenic assays and Western blot analysis tests further confirmed that compound 6 effectively induced apoptosis in HT-29 cells through mitochondrial- and caspase-3-dependent pathways.

Original languageEnglish
Article number2200486
Pages (from-to)e2200486
JournalArchiv der Pharmazie
Volume356
Issue number4
DOIs
StatePublished - 04 2023
Externally publishedYes

Bibliographical note

© 2022 Deutsche Pharmazeutische Gesellschaft.

Keywords

  • anticancer
  • chalcone
  • human colorectal adenocarcinoma cell
  • selenophene
  • Cell Proliferation
  • Humans
  • Structure-Activity Relationship
  • Chalcones/pharmacology
  • Chalcone
  • Selenium/pharmacology
  • Antineoplastic Agents/pharmacology
  • Cell Line, Tumor
  • Molecular Structure
  • Apoptosis
  • Drug Screening Assays, Antitumor

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