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

Chiba, Takuya  ,  Kitahata, Shun  ,  Matsuda, Akira  ,  Ichikawa, Satoshi

64 ( 7 )  , pp.811 - 816 , 2016-07 , The Pharmaceutical Society of Japan (日本薬学会)
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.

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