Drug intelligence / Profile preview

ophiobolin A C21-propyl ketone

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

Overview

Ophiobolin A C21-propyl ketone is a synthetic sesterterpenoid derivative of ophiobolin A, a natural product isolated from Bipolaris fungal species. It was designed to improve the metabolic stability of the parent compound by replacing the potentially labile C21-aldehyde group with a ketone. In preclinical studies, the compound was evaluated for its ability to target glioblastoma (GBM) and glioma stem cells (GSCs) through the induction of paraptosis, a form of non-apoptotic cell death. However, research indicates that the addition of the propyl group at the C21 position increases steric bulk, resulting in significantly reduced cytotoxic potency compared to the natural C21-aldehyde-containing ophiobolin A.

Other names
C21-propyl ophiobolin AC-21-propyl ophiobolin AC 21-propyl ophiobolin Aophiobolin A C21-Pr ketone
02

Targets

CaM (Calmodulin)PE (Phosphatidylethanolamine)PDE1 (Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase)

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