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Page 1
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
Martin MW, Newcomb J, Nunes JJ, Boucher C, Chai L, Epstein LF, Faust T, Flores S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Kim JL, Middleton S, Morgenstern K, Oliveira-dos-Santos A, Patel VF, Powers D, Rose P, Tudor Y, Turci SM, Welcher AA, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Ermann M, Johnston D, Saluste CG. Martin MW, et al. Among authors: middleton s. J Med Chem. 2008 Mar 27;51(6):1637-48. doi: 10.1021/jm701095m. Epub 2008 Feb 16. J Med Chem. 2008. PMID: 18278858
Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase.
Tamayo N, Liao L, Goldberg M, Powers D, Tudor YY, Yu V, Wong LM, Henkle B, Middleton S, Syed R, Harvey T, Jang G, Hungate R, Dominguez C. Tamayo N, et al. Among authors: middleton s. Bioorg Med Chem Lett. 2005 May 2;15(9):2409-13. doi: 10.1016/j.bmcl.2005.02.010. Bioorg Med Chem Lett. 2005. PMID: 15837335
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
Martin MW, Newcomb J, Nunes JJ, McGowan DC, Armistead DM, Boucher C, Buchanan JL, Buckner W, Chai L, Elbaum D, Epstein LF, Faust T, Flynn S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Lee JH, Metz D, Middleton S, Mohn D, Morgenstern K, Morrison MJ, Novak PM, Oliveira-dos-Santos A, Powers D, Rose P, Schneider S, Sell S, Tudor Y, Turci SM, Welcher AA, White RD, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Amouzegh P, Ermann M, Jenkins J, Johnston D, Napier S, Power E. Martin MW, et al. Among authors: middleton s. J Med Chem. 2006 Aug 10;49(16):4981-91. doi: 10.1021/jm060435i. J Med Chem. 2006. PMID: 16884310
Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.
Herberich B, Cao GQ, Chakrabarti PP, Falsey JR, Pettus L, Rzasa RM, Reed AB, Reichelt A, Sham K, Thaman M, Wurz RP, Xu S, Zhang D, Hsieh F, Lee MR, Syed R, Li V, Grosfeld D, Plant MH, Henkle B, Sherman L, Middleton S, Wong LM, Tasker AS. Herberich B, et al. Among authors: middleton s. J Med Chem. 2008 Oct 23;51(20):6271-9. doi: 10.1021/jm8005417. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817365
Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups.
Reed AB, Lanman BA, Neira S, Harrington PE, Sham KK, Frohn M, Pickrell AJ, Tasker AS, Gore A, Fiorino M, Itano A, McElvain M, Middleton S, Morrison H, Xu H, Xu Y, Wong M, Cee VJ. Reed AB, et al. Among authors: middleton s. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1779-83. doi: 10.1016/j.bmcl.2011.12.073. Epub 2011 Dec 21. Bioorg Med Chem Lett. 2012. PMID: 22257889
Analysis of the kinetics of osteoclastogenesis in arthritic rats.
Schett G, Stolina M, Bolon B, Middleton S, Adlam M, Brown H, Zhu L, Feige U, Zack DJ. Schett G, et al. Among authors: middleton s. Arthritis Rheum. 2005 Oct;52(10):3192-201. doi: 10.1002/art.21343. Arthritis Rheum. 2005. PMID: 16200623 Free article.
Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: potent S1P₁ agonists with in vivo lymphocyte-depleting activity.
Frohn M, Cee VJ, Lanman BA, Pickrell AJ, Golden J, Rivenzon-Segal D, Middleton S, Fiorino M, Xu H, Schrag M, Xu Y, McElvain M, Muller K, Siu J, Bürli R. Frohn M, et al. Among authors: middleton s. Bioorg Med Chem Lett. 2012 Jan 1;22(1):628-33. doi: 10.1016/j.bmcl.2011.10.069. Epub 2011 Oct 28. Bioorg Med Chem Lett. 2012. PMID: 22100314
Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5.
Cee VJ, Frohn M, Lanman BA, Golden J, Muller K, Neira S, Pickrell A, Arnett H, Buys J, Gore A, Fiorino M, Horner M, Itano A, Lee MR, McElvain M, Middleton S, Schrag M, Rivenzon-Segal D, Vargas HM, Xu H, Xu Y, Zhang X, Siu J, Wong M, Bürli RW. Cee VJ, et al. Among authors: middleton s. ACS Med Chem Lett. 2010 Dec 29;2(2):107-12. doi: 10.1021/ml100306h. eCollection 2011 Feb 10. ACS Med Chem Lett. 2010. PMID: 24900288 Free PMC article.
725 results