Synthetic studies on ligand molecules

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K07421
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Bioorganic chemistry
• Research Institution: Institute of Physical and Chemical Research
• Principal Investigator: Takahashi Shunya 国立研究開発法人理化学研究所, 環境資源科学研究センター, 専任研究員 (00202151)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: 分子リガンド / 天然物合成 / 生理活性天然物 / 酵素阻害剤 / 細胞毒性物質

Outline of Final Research Achievements

A ligand molecule that binds to a target protein is expected to be a useful tool for clarifying a variety of biofunctions. Bioactive natural products have been utilized as a model for designing a novel ligand molecule. In this project, p-terphenyls, steroids, and sugars are selected as the models, and basic studies based on the natural product synthesis were performed. Efficient methods for the syntheses of bioactive p-terphenyls such as polyozellin and kehokorins A-E were developed, thus leading to the structural revision of polyozellin and studies of the structure-activity relationship. Bioassay of newly designed p-terphenyls carrying a biotinyl unit was also examined with the aim of searching the target. For preparation of a ligand molecule utilizing an anticancer steroid as a model, chemical reactions of androsterone were investigated. A novel branched sugar was designed as a glycosidase inhibitor and was synthesized from D-glucose.

Free Research Field

天然物合成化学