8-methoxycoumarin-3-carboxylic acid

8-methoxycoumarin-3-carboxylic acid is a synthetic coumarin derivative investigated for its potential as an antineoplastic agent, specifically for the treatment of hepatocellular carcinoma (HCC). Identified as Compound 8 in preclinical research, it is synthesized via the hydrolysis of 8-methoxycoumarin-3-carboxamide. In *in vitro* evaluations using HepG2 liver cancer cells, the compound demonstrated significant antiproliferative activity with an IC50 of 5 µM, showing improved potency compared to its parent carboxamide. Its mechanism of action involves the inhibition of β-tubulin polymerization, which disrupts microtubule dynamics essential for cellular division and morphology, and the activation of executioner caspases (caspase-3 and caspase-7), leading to programmed cell death (apoptosis). Molecular modeling studies indicate that the compound possesses a high binding affinity for the active cavity of the β-tubulin protein, supporting its development as a microtubule-disrupting agent.

Other names

8-methoxy-2-oxo-2H-chromene-3-carboxylic acid