Related Experiment Video
Updated: Mar 12, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Design of chalcogen-containing norepinephrines: efficient GPx mimics and strong cytotoxic agents against HeLa cells
Azucena Marset1, Paloma Begines1, Óscar López1
1Departamento de Química Orgánica, Facultad de Química, Universidad de Sevilla, Apartado 1203, 41071, Seville, Spain.
Aim:
Numerous chronic diseases exhibit multifactorial etiologies, so focusing on a single therapeutic target is usually an inadequate treatment; instead, multi-target drugs are preferred. Herein, a panel of phenolic thioureas and selenoureas were designed as new prototypes against multifactorial diseases concerning antioxidation and cytotoxicity, as a pro-oxidant environment is usually found in such diseases.
Results:
Selenoureas were excellent antiradical agents and biomimetic catalysts of glutathione peroxidase for the scavenging of H2O2. They were also potent and selective cytotoxic agents against cancer cells, in particular HeLa (IC50 2.77-6.13 μM), apoptosis being involved. Selenoureas also reduced oxidative stress in HeLa cells (IC50= 3.76 μM).
Conclusion:
Phenolic selenoureas are promising lead structures for the development of drugs targeting multifactorial diseases like cancer.
More Related Videos
Related Concept Videos
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
Drugs Affecting Neurotransmitter Release or Uptake
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Drugs Acting on Autonomic Ganglia: Stimulants
Ganglionic stimulants activate NM nicotinic receptors in autonomic ganglia, falling into two categories: nicotine mimetics [e.g., lobeline, dimethylpiperazine, tetramethylammonium] and muscarinic receptor agonists [e.g., muscarine, methacholine]. The first category's action is rapid and blocked by nicotinic receptor antagonists, while the second category's action is delayed and blocked by atropine-like agents. Nicotine, an alkaloid, affects the heart rate by stimulating...
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
The direct-acting...
Adrenergic Agonists: Direct-Acting Agents
These agents can be classified...

