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2017 Fiscal Year Final Research Report

Development of new therapeutic agents derived from Wnt signaling inhibitor for treating brain cancer

Research Project

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Project/Area Number 15K14977
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Drug development chemistry
Research InstitutionOkayama University (2016-2017)
Osaka University (2015)

Principal Investigator

Yoshimitsu Takehiko  岡山大学, 医歯薬学総合研究科, 教授 (30301576)

Project Period (FY) 2015-04-01 – 2018-03-31
Keywordsアルカロイド / 脳腫瘍 / agelastatin A / Wnt/β-cateninシグナル阻害 / 抗がん剤 / 創薬
Outline of Final Research Achievements

Agelastatin A (AA) exhibits potent antiproliferative activity against cancer cell lines by inhibiting the Wnt/beta-catenin pathway responsible for cellular processes. The present study was undertaken to develop new therapeutic agents derived from AA for treating brain cancer and has culminated in the following achievements. 1) A new synthetic route to AA and AA derivatives was established by employing radical azidation of a silyl enol ether. The route enabled facile access to AA analogs with varying N1-substituents. Furthermore, AA analogs that exhibit potent inhibitory activity were identified by the structure-activity relationship (SAR) study. 2) A new method for the catalytic radical oxyazidation of alkenes was developed. 3) The divergent synthetic route successfully provided access to three chemical probes applicable for identifying the molecular target of AA. However, none of the probes were found to exert desirable activities.

Free Research Field

有機合成化学、創薬化学

URL: 

Published: 2019-03-29  

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