Design and synthesis of potent inhibitors of cholesteryl ester transfer protein (CETP) exploiting a 1, 2, 3, 4-tetrahydroquinoline platform

TA Rano, E Sieber-McMaster, PD Pelton…

Index: Rano, Thomas A.; Sieber-McMaster, Ellen; Pelton, Patricia D.; Yang, Maria; Demarest, Keith T.; Kuo, Gee-Hong Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 9 p. 2456 - 2460

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Citation Number: 57

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 IC50 of 39nM. The preparation of a series of potent inhibitors of CETP designed around a 1, 2, 3, 4- ...