Mechanisms
Tetrahydroquinoline platform yields a 39nM CETP inhibitor for raising HDL-C (Bioorg Med Chem Lett 2009)
Original title: Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform
Tetrahydroquinoline A, built around a 1,2,3,4-tetrahydroquinoline platform, inhibits partially purified cholesteryl ester transfer protein (CETP) with an IC50 of 39nM. CETP is presented as a target for treating low HDL-C and atherosclerosis alongside statins' LDL-C-lowering action. The paper describes the design and synthesis of a series of potent CETP inhibitors built on this tetrahydroquinoline scaffold.
Original abstract
Tetrahydroquinoline A is a potent inhibitor of the cholesterol ester transfer protein (CETP), a target for the treatment of low HDL-C and atherosclerosis. Low HDL-C has been identified as a key risk factor for cardiovascular disease in addition to high LDL-C, the target of the statin drugs. Tetrahydroquinoline A inhibits partially purified CETP with an IC(50) of 39nM. The preparation of a series of potent inhibitors of CETP designed around a 1,2,3,4-tetrahydroquinoline platform will be discussed.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.