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2014 Fiscal Year Final Research Report

A Novel Synthesis of Molecular-Targetting Indole Alkaloids and Elucidation of Anticancer Mechanism by Inducing Apoptosis

Research Project

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Project/Area Number 24590025
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Chemical pharmacy
Research InstitutionTokyo University of Science

Principal Investigator

KONAKAHARA Takeo  東京理科大学, 理工学部, 教授 (80084333)

Co-Investigator(Kenkyū-buntansha) SAKAI Norio  東京理科大学, 理工学部, 准教授 (00328569)
IKEDA Reiko  東京理科大学, 理工学部, 助教 (60516441)
AOKI Shin  東京理科大学, 薬学部, 教授 (00222472)
Project Period (FY) 2012-04-01 – 2015-03-31
Keywords抗がん剤 / β-カルボリン / エリプチシン / ピリジン / ピリミジン / アポトーシス / ヘテロ環合成 / フルオラス合成
Outline of Final Research Achievements

First, we have synthesized a series of new β-carboline derivatives, and evaluated their antitumor activity against HeLa S-3 cells to clarify its action mechanism and to provide its safety for a biological body using tumor-bearing mice. This compound acted as a tubulin polymerization inhibitor stronger than nocodazole, and suppressed the growth of the tumor of the mice. Glycosides and polyethylene glycol esters of many kinds of both β-carboline and ellipticine derivatives were also synthesized to evaluate their hydrophilicity and lipophilicity in connection with antitumor activity.
Second, we advocated a new concept of the fluorous-solid phase (FSP) synthesis, using a macroreticular fluorous polystyrene resin, as a sustainable organic synthesis. This new methodology provides both high reactivity as an advantage of a liquid-phase reaction and easy separation of the product as that of a solid-phase reaction. Finally, we applied it to the synthesis of β-carboline derivatives.

Free Research Field

医歯薬学

URL: 

Published: 2016-06-03  

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