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Lead biphenyl CETP inhibitor 12d significantly raises HDL in a transgenic mouse model (Bioorg Med Chem Lett 2010)

Original title: Design of a novel class of biphenyl CETP inhibitors

Bioorg Med Chem Lett · · 4

Lu Z, Napolitano JB, Theberge A, Ali A, Hammond ML, Tan E, Tong X, Xu SS, Latham MJ, Peterson LB, Anderson MS, Eveland SS et al.

Medicinal chemists designed and prepared a new class of biphenyl CETP inhibitors, potent both in vitro and in a cell-free assay and in vivo. The most active compound in the series, 12d, significantly raised HDL cholesterol in a transgenic mouse pharmacodynamic model, demonstrating that the biphenyl scaffold can translate direct CETP inhibitory potency into an in vivo lipid effect and adding another chemotype to the early-2010s CETP inhibitor discovery pipeline.

Read the paper (DOI)PubMed

Original abstract

A new class of CETP inhibitors was designed and prepared. These compounds are potent both in vitro and in vivo. The most active compound (12d) has shown an ability to raise HDL significantly in transgenic mouse PD model.

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Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.