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Page 1
Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model.
Julian LD, Wang Z, Bostick T, Caille S, Choi R, DeGraffenreid M, Di Y, He X, Hungate RW, Jaen JC, Liu J, Monshouwer M, McMinn D, Rew Y, Sudom A, Sun D, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP. Julian LD, et al. Among authors: degraffenreid m. J Med Chem. 2008 Jul 10;51(13):3953-60. doi: 10.1021/jm800310g. Epub 2008 Jun 14. J Med Chem. 2008. PMID: 18553955
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).
Sun D, Wang Z, Cardozo M, Choi R, Degraffenreid M, Di Y, He X, Jaen JC, Labelle M, Liu J, Ma J, Miao S, Sudom A, Tang L, Tu H, Ursu S, Walker N, Yan X, Ye Q, Powers JP. Sun D, et al. Among authors: degraffenreid m. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1522-7. doi: 10.1016/j.bmcl.2008.12.114. Epub 2009 Jan 9. Bioorg Med Chem Lett. 2009. PMID: 19181519
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors.
McMinn DL, Rew Y, Sudom A, Caille S, Degraffenreid M, He X, Hungate R, Jiang B, Jaen J, Julian LD, Kaizerman J, Novak P, Sun D, Tu H, Ursu S, Walker NP, Yan X, Ye Q, Wang Z, Powers JP. McMinn DL, et al. Among authors: degraffenreid m. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1446-50. doi: 10.1016/j.bmcl.2009.01.026. Epub 2009 Jan 15. Bioorg Med Chem Lett. 2009. PMID: 19185488
The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors.
Yan X, Wang Z, Sudom A, Cardozo M, DeGraffenreid M, Di Y, Fan P, He X, Jaen JC, Labelle M, Liu J, Ma J, McMinn D, Miao S, Sun D, Tang L, Tu H, Ursu S, Walker N, Ye Q, Powers JP. Yan X, et al. Among authors: degraffenreid m. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7071-5. doi: 10.1016/j.bmcl.2010.09.097. Epub 2010 Sep 29. Bioorg Med Chem Lett. 2010. PMID: 20971000
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors.
Sun D, Wang Z, Caille S, DeGraffenreid M, Gonzalez-Lopez de Turiso F, Hungate R, Jaen JC, Jiang B, Julian LD, Kelly R, McMinn DL, Kaizerman J, Rew Y, Sudom A, Tu H, Ursu S, Walker N, Willcockson M, Yan X, Ye Q, Powers JP. Sun D, et al. Among authors: degraffenreid m. Bioorg Med Chem Lett. 2011 Jan 1;21(1):405-10. doi: 10.1016/j.bmcl.2010.10.129. Epub 2010 Oct 31. Bioorg Med Chem Lett. 2011. PMID: 21093258
A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit.
Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Jaen JC, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Browner MF. Cushing TD, et al. Among authors: degraffenreid m. Bioorg Med Chem Lett. 2011 Jan 1;21(1):417-22. doi: 10.1016/j.bmcl.2010.10.126. Epub 2010 Oct 29. Bioorg Med Chem Lett. 2011. PMID: 21074993
A novel series of IKKβ inhibitors part II: description of a potent and pharmacologically active series of analogs.
Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Browner MF, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Jaen JC. Cushing TD, et al. Among authors: degraffenreid m. Bioorg Med Chem Lett. 2011 Jan 1;21(1):423-6. doi: 10.1016/j.bmcl.2010.10.125. Epub 2010 Oct 29. Bioorg Med Chem Lett. 2011. PMID: 21074992
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.
Brown ML, Aaron W, Austin RJ, Chong A, Huang T, Jiang B, Kaizerman JA, Lee G, Lucas BS, McMinn DL, Orf J, Rong M, Toteva MM, Xu G, Ye Q, Zhong W, Degraffenreid MR, Wickramasinghe D, Powers JP, Hungate R, Johnson MG. Brown ML, et al. Among authors: degraffenreid mr. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5206-9. doi: 10.1016/j.bmcl.2011.07.052. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21840217
14 results