A new concept for drug discovery from peptide natural products

2014 Fiscal Year Final Research Report

• Project/Area Number: 24659004
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Chemical pharmacy
• Research Institution: Kyoto University
• Principal Investigator: OISHI Shinya 京都大学, 薬学研究科(研究院), 講師 (80381739)
• Project Period (FY): 2012-04-01 – 2015-03-31
• Keywords: ペプチド / 二次代謝産物 / 天然物 / 全合成 / 薬らしさ

Outline of Final Research Achievements

Facile synthetic approaches to peptide natural products with multiple N-methyl amide bonds were investigated. For the synthesis of antiproliferative coibamide A, the solid-phase protocols were optimized. The macrolactonization of the linear precursor provided a coibamide A epimer with slightly less potent antiproliferative activity. Additionally, a facile synthetic process of IB-01212 via multiple N-methylation was established. The structure-activity relationship of a series of the derivatives revealed that the peptide conformation would mainly contribute to the bioactivity.

Free Research Field

創薬化学