Structure activity relationships study of dual-core type acetogenin analogues for development of novel antitumor agents

2016 Fiscal Year Final Research Report

• Project/Area Number: 25460159
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Kyoto Pharmaceutical University
• Principal Investigator: Kojima Naoto 京都薬科大学, 薬学部, 准教授 (90420413)
• Project Period (FY): 2013-04-01 – 2017-03-31
• Keywords: 抗がん剤 / 有機合成化学 / 構造活性相関研究 / 生物活性物質

Outline of Final Research Achievements

We reported that heterocycle-introduced analogues in the place of lactone ring as a common structure of annonaceous acetogenins, potently inhibit the growth of human cancer cell lines. Especially, a thiophen analog showed potent antitumor activity in in vivo assay using xenograft mice. In this work, we planned to synthesis of dual-core type analogues those have two heterocycles at the both ends of those. As a result, it was revealed that dual-core type analogue shows as potent inhibitory activity as the mother compound, indicating that dual-core type analogues may be a novel lead compound for antitumor agents.

Free Research Field

創薬化学