Michael R Degraffenreid

发表

Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.

N. Walker, Hiroshi Yamamoto, Zhulun Wang, 2008, Bioorganic & medicinal chemistry.

Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.

K. Pattabiraman, Zhulun Wang, C. Quéva, 2014, Journal of medicinal chemistry.

Improvement of the synthesis and pharmacokinetic properties of chromenotriazolopyrimidine MDM2-p53 protein-protein inhibitors.

J. Oliner, S. Olson, Q. Ye, 2011, Bioorganic & medicinal chemistry letters.

A novel series of IKKβ inhibitors part II: description of a potent and pharmacologically active series of analogs.

N. Walker, R. C. Hawley, C. Broka, 2011, Bioorganic & medicinal chemistry letters.

Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors.

N. Walker, R. Hungate, Zhulun Wang, 2009, Bioorganic & medicinal chemistry letters.

Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.

R. Hungate, M. Rong, W. Zhong, 2011, Bioorganic & medicinal chemistry letters.

Modulateurs d'inflammation

N. Walker, J. Jaén, J. Powers, 2002 .

An Efficient and Scalable One-Pot Double Michael Addition-Dieckmann Condensation for the Synthesis of 4,4-Disubstituted Cyclohexane β-Keto Esters

R. Hungate, J. Powers, D. McMinn, 2007 .

The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors.

N. Walker, Zhulun Wang, Jinsong Liu, 2010, Bioorganic & medicinal chemistry letters.

A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit.

N. Walker, R. C. Hawley, C. Broka, 2011, Bioorganic & medicinal chemistry letters.

Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model.

M. Monshouwer, N. Walker, R. Hungate, 2008, Journal of medicinal chemistry.

Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11β-HSD1 inhibitors.

J. Jaén, J. Powers, D. McMinn, 2012, Bioorganic & medicinal chemistry letters.

Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).

N. Walker, Zhulun Wang, Jinsong Liu, 2009, Bioorganic & medicinal chemistry letters.

Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors.

N. Walker, R. Hungate, Zhulun Wang, 2011, Bioorganic & medicinal chemistry letters.

Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.

K. Pattabiraman, Zhulun Wang, C. Quéva, 2014, Journal of medicinal chemistry.

Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.

R. Hungate, M. Rong, W. Zhong, 2011, Bioorganic & medicinal chemistry letters.