Lipophilic Isosteres of a pi-pi Stacking Interaction: New Inhibitors of the Bcl-2-Bak Protein-Protein Interaction

[摘要]：The discovery of new Bcl-2 protein-protein interaction antagonists is described. We replaced the northern fragment of ABT737 (pi-pi stacking interactions) with structurally simplified hydrophobic cage structures with much reduced conformational flexibility and rotational freedom. The binding mode of the compounds was elucidated by X-ray crystallography, and the compounds showed excellent oral bioavailability and clearance in rat PK studies.

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