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

Arch Pharm (Weinheim). 2023 Apr;356(4):e2200486. doi: 10.1002/ardp.202200486. Epub 2023 Jan 1.

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.

Keywords: anticancer; chalcone; human colorectal adenocarcinoma cell; selenophene.

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Apoptosis
  • Cell Line, Tumor
  • Cell Proliferation
  • Chalcone*
  • Chalcones* / pharmacology
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Selenium* / pharmacology
  • Structure-Activity Relationship

Substances

  • Chalcone
  • Chalcones
  • Selenium
  • Antineoplastic Agents