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Updated: Mar 18, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Design, Synthesis and Biological Evaluation of a Structurally Simplified Syringolin A Analogues
Takuya Chiba1, Shun Kitahata, Akira Matsuda
1Faculty of Pharmaceutical Science, Hokkaido University.
Abstract:
In this study, we designed and synthesized a structurally simplified syringolin A analogue 4, which could have a switched hydrogen bonding interaction with the β5 subunit of 20S proteasome. This analogue exhibits potent β5 proteasome inhibitory activity with an IC50 value of 107 nM. It also shows cytotoxicity against a range of human cancer cells at submicromolar level (109-254 nM). This analogue is expected to be a lead compound as a next generation proteasome inhibitor because of its simple structure.
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