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Updated: Jun 7, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors
Xuelei Yan1, Zhulun Wang, Athena Sudom
1Amgen Inc., 1120 Veterans Boulevard, South San Francisco, CA 94080, USA. xueleiy@amgen.com
Abstract:
In this communication, human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11β-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent efficacy in a non-human primate ex vivo pharmacodynamic model.
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