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2016 Fiscal Year Final Research Report

Development of nobel anti-myeloma agent based on natural macrolide

Research Project

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Project/Area Number 15K18830
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Chemical pharmacy
Research InstitutionThe University of Tokushima

Principal Investigator

NAKAYAMA Atsushi  徳島大学, 大学院医歯薬学研究部(薬学系), 助教 (60743408)

Project Period (FY) 2015-04-01 – 2017-03-31
Keywords天然マクロライド / 多発性骨髄腫
Outline of Final Research Achievements

LL-Z1640-2 (1) is a member of 14-membered macrolide containing cis-enone moiety . This is known as a potent and selective TAK-1 (TGF-b activated kinase 1) inhibitor. Recently, we revealed that 1 exhibited a marked tumor reduction effect for multiple myeloma(MM)-bearing mice. Moreover the osteolytic bone destruction which is caused in MM was also suppressed by the administration of LL-Z1640-2. Although LL-Z1640-2 can be considered as a promising seed molecule of antitumor drug, the supplement of it is not stable for the further animal experiments. To facilitate the development of anti-MM agent, the establishment of the novel synthetic route of LL-Z1640-2 was conducted. This synthesis involved a ring-closing metathesis under low temperature as a key reaction and last stage isomerization from cis-enone to trans-enone. As a result, four derivatives including LL-Z1640-2 were obtained throughout this total synthesis and we also discovered some derivatives which have potent anti-MM agents.

Free Research Field

有機合成化学

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Published: 2018-03-22  

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