Design, synthesis, and biological antitumor evaluation of tetrahydroisoquinoline derivatives

Bioorg Med Chem Lett. 2024 Sep 1:109:129824. doi: 10.1016/j.bmcl.2024.129824. Epub 2024 May 31.

Abstract

Cancer, as a public health issue, is the leading cause of death worldwide. Tetrahydroisoquinoline derivatives have effective biological activities and can be used as potential therapeutic agents for antitumor drugs. In this work, we designed and synthesized a series of novel tetrahydroisoquinoline compounds and evaluated their antitumor activity in vitro on several representative human cancer cell lines. The results showed that the vast majority of compounds showed good inhibitory activities against the cancer cell lines of HCT116, MDA-MB-231, HepG2, and A375.

Keywords: Antitumor; In vitro; Quaternary ammonium salt; Synthesis; Tetrahydroisoquinoline.

MeSH terms

  • Antineoplastic Agents* / chemical synthesis
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Drug Screening Assays, Antitumor*
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship
  • Tetrahydroisoquinolines* / chemical synthesis
  • Tetrahydroisoquinolines* / chemistry
  • Tetrahydroisoquinolines* / pharmacology

Substances

  • Tetrahydroisoquinolines
  • Antineoplastic Agents