1-acetyl-5-amino-4-(2-oxo-2h-chromene-6-sulfonyl)-1,2-dihydro-pyrazol-3-one

1-acetyl-5-amino-4-(2-oxo-2h-chromene-6-sulfonyl)-1,2-dihydro-pyrazol-3-one, also referred to as compound 4 in research studies, is a synthetic small molecule sulfonyl coumarin derivative designed as a non-cytotoxic anti-angiogenic agent. Developed by researchers at the National Research Centre in Egypt, it is primarily investigated for its potential in treating hepatocellular carcinoma. The compound's mechanism of action involves the inhibition of tumor cell migration through a matrix metalloproteinase (MMP)-dependent pathway, specifically targeting MMP-2, and the down-regulation of CD105 (endoglin), a key co-receptor for TGF-beta involved in angiogenesis. Molecular docking studies indicate that the molecule fits into the active site of MMP-2, forming ionic interactions with the catalytic zinc ion and hydrogen bonds with residues such as Leu83 and Glu121. Its non-cytotoxic profile makes it a candidate for targeted molecular therapy, potentially avoiding the systemic toxicity associated with conventional cytotoxic drugs.

Other names

1-acetyl-5-amino-4-(2-oxo-2H-chromene-6-sulfonyl)-1,2-dihydropyrazol-3-one