Development of lamellarin type axially chiral molecules aiming at the creation of selective kinase inhibitors

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K01802
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Biomolecular chemistry
• Research Institution: Nagasaki University
• Principal Investigator: FUKUDA Tsutomu 長崎大学, 工学研究科, 助教 (80295097)
• Co-Investigator(Renkei-kenkyūsha): SHIGEMITSU Yasuhiro 長崎大学, 工学研究科, 准教授 (50432969)
• Project Period (FY): 2015-04-01 – 2018-03-31
• Keywords: ラメラリン / 軸不斉 / アトロプ異性体 / プロテインキナーゼ / ハロゲン化

Outline of Final Research Achievements

Axially chiral 16-chloro and 16-bromolamellarins N have been developed for the creation of selective kinase inhibitors. The kinase inhibitory activities of these enantiomers were evaluated on seven protein kinases. The (aR)-isomers of 16-chloro and 16-bromolamellarins N exhibited potent but non-selective inhibition on five protein kinases except for CK1ε and CLK3. On the other hand, the (aS)-isomers showed selective inhibition against only DYRK1A, GSK-3β, and PIM1.

Free Research Field

有機合成化学、創薬化学