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sodium (3β-hydroxy-(17R)-17-28-norlup-20(29)-en)-2-oxoethyl-phosphonate
- Development stage
- Preclinical
- Modality
- Small Molecules
01
Overview
sodium (3β-hydroxy-(17R)-17-28-norlup-20(29)-en)-2-oxoethyl-phosphonate is a semisynthetic pentacyclic triterpenoid derivative of betulinic acid. It features a methylphosphonate moiety attached to the C17 position, designed to optimize the pharmacokinetic and pharmacodynamic profiles of the parent triterpene. In preclinical evaluations using the B164A5 murine melanoma cell line, the compound demonstrated dose-dependent antiproliferative and anti-migratory activities. Mechanistically, it appears to induce apoptosis, as evidenced by nuclear condensation in Hoechst 33342 staining, while maintaining a low cytotoxicity profile similar to its parent compound (betulinic acid). Biocompatibility studies using the HET-CAM assay have indicated that the compound does not cause significant vascular disintegration, hemorrhage, or coagulation, suggesting potential for further development as an antimelanoma agent.
- Other names
- sodium salt of betulinic acid phosphonomethyl esterbetulinic acid phosphonate derivative
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