Drug intelligence / Profile preview

8-methoxycoumarin-3-carboxamide

Development stage
Preclinical
Lead developer
Shaqra University
Modality
Small Molecules
01

Overview

8-methoxycoumarin-3-carboxamide is a synthetic coumarin-based small molecule investigated for its potential therapeutic application in hepatocellular carcinoma (HCC). It serves as the parent scaffold for a novel series of N-(substituted-phenyl)-8-methoxycoumarin-3-carboxamides designed to target liver cancer cells. The compound demonstrates moderate antiproliferative activity against HepG2 cells, while its derivatives, such as the 5-bromo analogue (Compound 5), exhibit significantly higher potency. Its mechanism of action involves the activation of executioner caspases (Caspase-3 and Caspase-7) and the inhibition of β-tubulin polymerization. By disrupting microtubule dynamics and triggering the apoptotic pathway, the compound induces cell cycle arrest (typically in the G1/S or G2/M phases) and programmed cell death in neoplastic cells with minimal impact on normal healthy cells.

Other names
8-methoxy-2-oxo-2H-chromene-3-carboxamide
02

Targets

CASP7 (Caspase-7)CASP3 (Caspase-3)TUBB (Tubulin (alpha and beta subunits))

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