Related Experiment Video
Updated: May 25, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Function Oriented Synthesis: Preparation and Initial Biological Evaluation of New A-Ring-Modified Bryologs
1Department of Chemistry, Department of Chemical and Systems Biology, Stanford University, Stanford, California 94305-5080, USA.
Abstract:
The synthesis and biological evaluation of the first members of a new series of designed bryostatin A-ring analogues (bryologs) are described. An advanced intermediate is produced that allows for step economical access to diverse analogs. The first of these analogues, bearing side chains of completely different polarities from alkyl to hydroxyl and carboxyl functionalities, were evaluated. All exhibit potent protein kinase C binding (54.7 to 2.4 nM) with affinities increasing with decreasing side chain polarity. This series of bryostatin analogues demonstrates that A ring surrogates can indeed be used for tuning pharmacophore and ADME characteristics as needed to improve bryolog function.
More Related Videos
Related Concept Videos
Synthetic Biology
Golden rice
Golden rice is a genetically modified...
Base-Catalyzed Ring-Opening of Epoxides
Olefin Metathesis Polymerization: Ring-Opening Metathesis Polymerization (ROMP)
ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH3
Acid-Catalyzed Ring-Opening of Epoxides
Drug Discovery: Overview

