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sodium (3β-hydroxy-(17r)-17-28-norolean-12(13)-en)-2-oxoethyl-phosphonate
- Development stage
- Preclinical
- Modality
- Small Molecules
01
Overview
sodium (3β-hydroxy-(17r)-17-28-norolean-12(13)-en)-2-oxoethyl-phosphonate is a semisynthetic derivative of the natural pentacyclic triterpenoid oleanolic acid. It was developed with a methylphosphonate moiety at the C17 position to enhance the pharmacokinetic and pharmacodynamic profiles of the parent compound, which typically exhibits poor bioavailability. In preclinical evaluations using the B164A5 murine melanoma cell line, this compound demonstrated significant dose-dependent antiproliferative and anti-migratory activity. It appears to induce apoptosis, as evidenced by increased nuclear condensation, while maintaining a favorable safety profile with no significant cytotoxicity to non-cancerous cells in LDH and HET-CAM assays.
- Other names
- oleanolic acid phosphonomethyl ester sodium saltsodium {[(3β-hydroxyolean-12-en-28-oyl)oxy]methyl}phosphonate
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