1335147-11-9Relevant academic research and scientific papers
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
supporting information; experimental part, 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.
APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES
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Page/Page column 36, (2011/10/12)
Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
