Discovering novel 7-azaindole-based series as potent AXL kinase inhibitors
AXL is a receptor tyrosine kinase that plays a key role in tumor growth and proliferation. The scientific community has validated AXL as therapeutic target in the treatment of cancers for several years now, and several AXL inhibitors have been developed but none of them are approved. In this context, we started to design new kinase inhibitors targeting AXL from the 7-azaindole scaffold well known to interact with the ATP binding site of the kinase. Focused screening and chemical diversification around 7-azaindole scaffold were developed, based on modeling studies and medicinal chemistry rational, leading to the discovery of a new family of hits with potent inhibitory activity against AXL.
Design and synthesis of orally bioavailable serum and glucocorticoid-regulated kinase 1 (SGK1) inhibitors
The lead serum and glucocorticoid-related kinase 1 (SGK1) inhibitors 4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid (1) and {4-[5-(2-naphthalenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]phenyl}acetic acid (2) suffer from low DNAUC values in rat, due in par
Hammond, Marlys,Washburn, David G.,Hoang, Tram H.,Manns, Sharada,Frazee, James S.,Nakamura, Hiroko,Patterson, Jaclyn R.,Trizna, Walter,Wu, Charlene,Azzarano, Leonard M.,Nagilla, Rakesh,Nord, Melanie,Trejo, Rebecca,Head, Martha S.,Zhao, Baoguang,Smallwood, Angela M.,Hightower, Kendra,Laping, Nicholas J.,Schnackenberg, Christine G.,Thompson, Scott K.
experimental part
p. 4441 - 4445
(2010/04/05)
1H-PYRROLO[2,3-B]PYRIDINES
Derivatives of pyrrolo[2,3-b]pyridine which are useful as SGK-1 kinase inhibitors are described herein. The invention described herein also describes pharmaceutical compositions containing derivatives of pyrrolo[2,3-b]pyridine and methods of using pyrrolo[2,3-b]pyridine derivatives and pharmaceutical compositions thereof in the treatment of diseases mediated by SGK-1.
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Page/Page column 35
(2008/06/13)
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