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3-oxo-(17s)-17-(((dimethoxyphosphoryl)methoxy)carbonyl)-28-norlup-20(29)-ene

Development stage
Preclinical
Modality
Small Molecules
01

Overview

3-oxo-(17s)-17-(((dimethoxyphosphoryl)methoxy)carbonyl)-28-norlup-20(29)-ene is a semisynthetic pentacyclic triterpenoid derivative of betulonic acid (the 3-oxo analog of betulinic acid). It features a methylphosphonate moiety (dimethoxyphosphorylmethoxycarbonyl) at the C-17 position, a modification designed to enhance the pharmacokinetic properties and bioavailability of the parent triterpenoid scaffold. In preclinical evaluations against the B164A5 murine melanoma cell line, the compound demonstrated significant dose-dependent antiproliferative and anti-migratory activities. It is being investigated as a potential antimelanoma strategy due to its ability to reduce cell viability without inducing significant non-specific cytotoxicity, as evidenced by LDH assays and HET-CAM vascular safety testing.

Other names
Betulonic acid dimethoxyphosphorylmethyl ester3-oxobetulinic acid dimethoxyphosphorylmethyl ester

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