Seed compounds exploratory empowered by catalysis
| Project/Area Number |
18K19156
|
|---|
| Research Category |
Grant-in-Aid for Challenging Research (Exploratory)
|
| Allocation Type | Multi-year Fund |
|---|
| Review Section |
Medium-sized Section 37:Biomolecular chemistry and related fields
|
|---|
| Research Institution | Institute of Physical and Chemical Research |
|---|
Principal Investigator |
SOHTOME Yoshihiro 国立研究開発法人理化学研究所, 開拓研究本部, 専任研究員 (50431888)
|
|---|
| Project Period (FY) |
2018-06-29 – 2022-03-31
|
| Project Status |
Completed (Fiscal Year 2021)
|
| Budget Amount *help |
¥6,240,000 (Direct Cost: ¥4,800,000、Indirect Cost: ¥1,440,000)
Fiscal Year 2020: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
Fiscal Year 2019: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
Fiscal Year 2018: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
|
|---|
| Keywords | 分子触媒 / 含窒素化合物 / 複素環化合物 / 連続不斉炭素 / 四級炭素 / 生物活性 / 抗感染症剤 / シード化合物 / 有機合成化学 / 不斉触媒 / 酵素 / プロテオミクス / ヘテロ原子 / 触媒 |
|---|
| Outline of Final Research Achievements |
The primary aim of this project is to identify new classes of biologically active molecules on the bais of the originally developed catalysis. We have developed catalytic strategies to efficiently construct the complex molecules having the sp3-rich scaffold, especially focusing on higher oxidation states, contiguous stereocenters, and quaternary carbons. Among the 700 compounds (including products, starting materials, intermediates, and ligands), we identified the several new compounds, which exhibit unique biological activities with less toxicity. For new seed compounds, we examined the concentration effect to obtain the IC50 value, toxicity test, and structure-activity relationship studies.
|
| Academic Significance and Societal Importance of the Research Achievements |
生体分子の機能をより選択的に制御する低分子化合物の創出は、世界有数の少子高齢化社会に突入する我が国において、永続的に取り組むべき課題である。しかしながら、物質化学的興味に触発され、アカデミアで合成された人工分子の多くは、製薬会社が追求するドラックライクネス (リピンスキー則等) の指標から外れている場合が多い。そのため、これらの合成分子は、シード化合物としての可能性は十分に検討されてこなかった。一方、本研究では、独自の化合物ライブラリーの構築、生物活性評価、構造展開研究を有機的に連動させることで、ユニークな生物活性シードを創出できることが示された。
|
Report
(5 results)
Research Products
(39 results)
-
-
-
-
-
-
-
-
-
-
-
[Journal Article] Unveiling epidithiodiketopiperazine as a non-histone arginine methyltransferase inhibitor by chemical protein methylome analyses2018
Author(s)
Yoshihiro Sohtome, Tadahiro Shimazu, Joaquin Barjau, Shinya Fujishiro, Mai Akakabe, Naoki Terayama, Kosuke Dodo, Akihiro Ito, Minoru Yoshida, Yoichi Shinkai, Mikiko Sodeoka
-
Journal Title
Chem. Commun.
Volume: 54
Issue: 66
Pages: 9202-9205
DOI
Related Report
Peer Reviewed / Int'l Joint Research
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
