Drug intelligence / Profile preview

C20-oxosalinomycin benzhydroxamic acid

Development stage
Preclinical
Lead developer
Adam Mickiewicz University
Modality
Small Molecules
01

Overview

C20-oxosalinomycin benzhydroxamic acid (also known as compound 17) is a semi-synthetic, double-modified analog of the polyether ionophore antibiotic salinomycin. It is generated by the chemoselective oxidation of the C20 allylic hydroxyl of salinomycin to a ketone (C20-oxo) and conjugation with benzhydroxamic acid at the C1 carboxyl position. Developed by researchers at Adam Mickiewicz University and the University of Arkansas for Medical Sciences, this compound is designed to target cancer stem cells (CSCs) with improved potency and selectivity compared to parent salinomycin. It has demonstrated significant in vitro and 3D organoid efficacy against breast cancer stem cells (specifically the CD44+/CD24- subpopulation) and various other tumor cell lines in the NCI-60 panel. Its mechanism of action involves the induction of apoptosis, characterized by DNA fragmentation, PARP cleavage, and downregulation of the anti-apoptotic protein Bcl-2.

Other names
C20-oxosalinomycin benzhydroxamateC-20-oxosalinomycin benzhydroxamateC 20-oxosalinomycin benzhydroxamatedouble-modified C20-oxosalinomycin with benzhydroxamic acid
02

Targets

BCL-2 (BCL-2 family)

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