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


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Please use this identifier to cite or link to this item:http://hdl.handle.net/2115/62874

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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