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Design, Synthesis and Biological Evaluation of a Structurally Simplified Syringolin A Analogues

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Title: Design, Synthesis and Biological Evaluation of a Structurally Simplified Syringolin A Analogues
Authors: Chiba, Takuya Browse this author
Kitahata, Shun Browse this author
Matsuda, Akira Browse this author →KAKEN DB
Ichikawa, Satoshi Browse this author →KAKEN DB
Keywords: proteasome
natural product
anticancer
Issue Date: Jul-2016
Publisher: The Pharmaceutical Society of Japan
Journal Title: Chemical & pharmaceutical bulletin
Volume: 64
Issue: 7
Start Page: 811
End Page: 816
Publisher DOI: 10.1248/cpb.c16-00182
PMID: 27373636
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 beta 5 subunit of 20S proteasome. This analogue exhibits potent beta 5 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.
Type: article
URI: http://hdl.handle.net/2115/62874
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 市川 聡

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