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3-oxo-(17s)-17-(((dimethoxyphosphoryl)methoxy)carbonyl)-28-norurs-12(13)-ene

Development stage
Preclinical
Lead developer
Victor Babeș University of Medicine and Pharmacy Timișoara
Modality
Small Molecules
01

Overview

3-oxo-(17s)-17-(((dimethoxyphosphoryl)methoxy)carbonyl)-28-norurs-12(13)-ene is a semisynthetic pentacyclic triterpenoid derivative of ursonic acid (the 3-oxo derivative of ursolic acid). It features a methylphosphonate moiety introduced at the C17 position via an ester linkage, a modification intended to optimize the pharmacokinetic and pharmacodynamic profiles of natural triterpenoids. In preclinical evaluations, this specific derivative has demonstrated dose-dependent antiproliferative and anti-migratory activity against the B164A5 murine melanoma cell line. The compound appears to induce apoptosis, as evidenced by nuclear condensation, while maintaining a favorable safety profile with no significant increase in non-specific cytotoxicity or vascular disintegration observed in LDH and HET-CAM assays, respectively.

Other names
ursonic acid methylphosphonate derivativedimethoxyphosphorylmethyl ursonate

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