Orally bioavailable antagonists of inhibitor of apoptosis proteins based on an azabicyclooctane scaffold
A series of IAP antagonists based on an azabicyclooctane scaffold was designed and synthesized. The most potent of these compounds, 14b, binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domain of c-IAP1 with Ki values of 14
Cohen, Frederick,Alicke, Bruno,Elliott, Linda O.,Flygare, John A.,Goncharov, Tatiana,Keteltas, Stephen F.,Franklin, Matthew C.,Frankovitz, Stacy,Stephan, Jean-Philippe,Tsui, Vickie,Vucic, Domagoj,Wong, Harvey,Fairbrother, Wayne J.
experimental part
p. 1723 - 1730
(2010/02/28)
AZABICYCLO-OCTANE INHIBITORS OF IAP
The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula (I) in which X1 and X2 are independently O or S; L is a bond or -C(X3
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Page/Page column 38
(2008/06/13)
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