Drug intelligence / Profile preview

ophiobolin A C21-isopropyl ketone

Development stage
Preclinical
Lead developer
Texas State University
Modality
Small Molecules
01

Overview

Ophiobolin A C21-isopropyl ketone is a synthetic analog of ophiobolin A, a sesterterpenoid fungal metabolite isolated from *Bipolaris* species. Developed by researchers at Texas State University and collaborating institutions, this compound was designed to investigate the structure-activity relationship of the C21-aldehyde group, which is a potential metabolic liability in the parent molecule. Ophiobolin A is known to exhibit potent cytotoxicity against glioblastoma (GBM) and glioma stem cells (GSCs) by inducing paraptosis, characterized by cytoplasmic vacuolization. However, the C21-isopropyl ketone derivative demonstrated inferior potency compared to the natural aldehyde, suggesting that increasing steric bulk at the C21 position negatively impacts the compound's ability to induce cell death in glioma models.

Other names
ophiobolin A C21-isopropyl ketone
02

Targets

PE (Phosphatidylethanolamine)

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