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Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
Pennington LD, Croghan MD, Sham KK, Pickrell AJ, Harrington PE, Frohn MJ, Lanman BA, Reed AB, Lee MR, Xu H, McElvain M, Xu Y, Zhang X, Fiorino M, Horner M, Morrison HG, Arnett HA, Fotsch C, Tasker AS, Wong M, Cee VJ. Pennington LD, et al. Among authors: xu h, xu y. Bioorg Med Chem Lett. 2012 Jan 1;22(1):527-31. doi: 10.1016/j.bmcl.2011.10.085. Epub 2011 Nov 4. Bioorg Med Chem Lett. 2012. PMID: 22104144
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: xu h, xu y. 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
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: xu h, xu y. 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
4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1.
Pennington LD, Sham KK, Pickrell AJ, Harrington PE, Frohn MJ, Lanman BA, Reed AB, Croghan MD, Lee MR, Xu H, McElvain M, Xu Y, Zhang X, Fiorino M, Horner M, Morrison HG, Arnett HA, Fotsch C, Wong M, Cee VJ. Pennington LD, et al. Among authors: xu h, xu y. ACS Med Chem Lett. 2011 Jul 29;2(10):752-7. doi: 10.1021/ml2001399. eCollection 2011 Oct 13. ACS Med Chem Lett. 2011. PMID: 24900263 Free PMC article.
Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core.
Harrington PE, Croghan MD, Fotsch C, Frohn M, Lanman BA, Pennington LD, Pickrell AJ, Reed AB, Sham KK, Tasker A, Arnett HA, Fiorino M, Lee MR, McElvain M, Morrison HG, Xu H, Xu Y, Zhang X, Wong M, Cee VJ. Harrington PE, et al. Among authors: xu h, xu y. ACS Med Chem Lett. 2011 Nov 23;3(1):74-8. doi: 10.1021/ml200252b. eCollection 2012 Jan 12. ACS Med Chem Lett. 2011. PMID: 24900374 Free PMC article.
The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.
Wang HL, Cee VJ, Chavez F Jr, Lanman BA, Reed AB, Wu B, Guerrero N, Lipford JR, Sastri C, Winston J, Andrews KL, Huang X, Lee MR, Mohr C, Xu Y, Zhou Y, Tasker AS. Wang HL, et al. Among authors: xu y. Bioorg Med Chem Lett. 2015 Feb 15;25(4):834-40. doi: 10.1016/j.bmcl.2014.12.068. Epub 2014 Dec 30. Bioorg Med Chem Lett. 2015. PMID: 25597005
Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors.
Wurz RP, Sastri C, D'Amico DC, Herberich B, Jackson CLM, Pettus LH, Tasker AS, Wu B, Guerrero N, Lipford JR, Winston JT, Yang Y, Wang P, Nguyen Y, Andrews KL, Huang X, Lee MR, Mohr C, Zhang JD, Reid DL, Xu Y, Zhou Y, Wang HL. Wurz RP, et al. Among authors: xu y. Bioorg Med Chem Lett. 2016 Nov 15;26(22):5580-5590. doi: 10.1016/j.bmcl.2016.09.067. Epub 2016 Oct 1. Bioorg Med Chem Lett. 2016. PMID: 27769621
Discovery of amido-benzisoxazoles as potent c-Kit inhibitors.
Kunz RK, Rumfelt S, Chen N, Zhang D, Tasker AS, Bürli R, Hungate R, Yu V, Nguyen Y, Whittington DA, Meagher KL, Plant M, Tudor Y, Schrag M, Xu Y, Ng GY, Hu E. Kunz RK, et al. Among authors: xu y. Bioorg Med Chem Lett. 2008 Sep 15;18(18):5115-7. doi: 10.1016/j.bmcl.2008.07.111. Epub 2008 Jul 31. Bioorg Med Chem Lett. 2008. PMID: 18723346
73,231 results
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