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Updated: Aug 26, 2025

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Published on: May 28, 2014

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Structure-activity relationships of mixed σ1R/σ2R ligands with antiproliferative and anticancer effects

Antonino N Fallica1, Valeria Ciaffaglione1, Maria N Modica1

  • 1Department of Drug and Health Sciences, University of Catania, viale A. Doria 6, 95125, Catania, Italy.

Bioorganic & Medicinal Chemistry
|October 6, 2022
PubMed

Insights

Sigma receptors (σRs) are overexpressed in tumors, making σR ligands promising anticancer agents. These ligands inhibit cancer cell growth and migration, and are also used for imaging tumors.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Overexpression of sigma receptors (σRs) in tumors suggests a role in cancer.
  • σR ligands are investigated as potential chemotherapeutics due to their antiproliferative effects.

Purpose of the Study:

  • To review recent advances in the development of sigma receptor (σR) ligands.
  • To describe structure-activity relationships of mixed σ1R/σ2R ligands with antitumor potential.

Main Methods:

  • Literature review of recent studies on σR ligands.
  • Analysis of structure-activity relationships for mixed σ1R/σ2R ligands.

Main Results:

  • σR ligands inhibit cancer cell survival, migration, and proliferation by modulating tumorigenic pathways.
  • Structurally diverse mixed σ1R/σ2R ligands show promising antitumor activity against various cancer cell lines.
  • σR ligands are also explored as radiotracers for PET and SPECT imaging.

Conclusions:

  • σR ligands represent a novel class of chemotherapeutic agents with dual roles in cancer treatment and imaging.
  • Further development of σR ligands is warranted for their clinical application in oncology.
Keywords:
Antiproliferative activityCancerσ Receptor ligandsσ Receptorsσ(1) Receptorσ(2) Receptor

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