Drug intelligence / Profile preview

n-acetyl 5-bromo-8-methoxycoumarin-3-carboxamide

Development stage
Preclinical
Lead developer
Shaqra University
Modality
Small Molecules
01

Overview

n-acetyl 5-bromo-8-methoxycoumarin-3-carboxamide is an experimental small molecule coumarin derivative developed for the treatment of hepatocellular carcinoma. It belongs to a novel series of 8-methoxycoumarin-3-carboxamides designed to target cancer cell proliferation. Mechanistically, this class of compounds acts by inhibiting β-tubulin polymerization, which disrupts microtubule dynamics and leads to cell cycle arrest (specifically at the G2/M phase). Additionally, these compounds trigger apoptosis through the activation of executioner caspases, specifically caspase-3 and caspase-7. In preclinical assays using HepG2 liver cancer cells, this specific acetylated derivative demonstrated significant antiproliferative activity with an IC50 of 2.3 µM, although it was slightly less potent than its non-acetylated precursor (Compound 5).

Other names
N-acetyl 5-bromo-8-methoxycoumarin-3-carboxamideN-acetyl5-bromo-8-methoxycoumarin-3-carboxamideN-acetyl-5-bromo-8-methoxycoumarin-3-carboxamide
02

Targets

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

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