1382034-66-3Relevant articles and documents
Lipophilic isosteres of a π-π Stacking interaction: New inhibitors of the Bcl-2-Bak protein-protein interaction
Yusuff, Naeem,Dore, Michael,Joud, Carol,Visser, Michael,Springer, Clayton,Xie, Xiaoling,Herlihy, Kara,Porter, Dale,Toure, B. Barry
, p. 579 - 583 (2012/09/08)
The discovery of new Bcl-2 protein-protein interaction antagonists is described. We replaced the northern fragment of ABT737 (π-π 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.