Drug intelligence / Profile preview

ligand-L

Development stage
Preclinical
Lead developer
Ligand Pharmaceuticals
Modality
Small Molecules
01

Overview

ligand-L is a synthesized coumarin-based copper chelator designed for targeted cancer therapy. It functions by chelating elevated copper levels found in malignant cells, leading to redox cycling of copper and subsequent generation of reactive oxygen species (ROS). This cascade results in DNA damage, loss of mitochondrial membrane potential, and activation of caspase-3, ultimately inducing apoptosis in cancer cells. Its anticancer activity has been demonstrated in a rat model of diethylnitrosamine-induced hepatocellular carcinoma, showing improvements in liver marker enzymes, liver surface morphology, and reduced alpha-fetoprotein levels.

Other names
di(2-picolyl)amine-3(bromoacetyl)coumarin hybrid molecule
02

Targets

CASP3 (Caspase-3)DNA

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