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  • Title: Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1,2,3,4-tetrahydroquinoline platform.
    Author: Rano TA, Sieber-McMaster E, Pelton PD, Yang M, Demarest KT, Kuo GH.
    Journal: Bioorg Med Chem Lett; 2009 May 01; 19(9):2456-60. PubMed ID: 19339179.
    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.
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