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Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).
Gonzalez-Lopez de Turiso F, Hao X, Shin Y, Bui M, Campuzano ID, Cardozo M, Dunn MC, Duquette J, Fisher B, Foti RS, Henne K, He X, Hu YL, Kelly RC, Johnson MG, Lucas BS, McCarter J, McGee LR, Medina JC, Metz D, San Miguel T, Mohn D, Tran T, Vissinga C, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Gonzalez-Lopez de Turiso F, et al. Among authors: johnson mg. J Med Chem. 2016 Aug 11;59(15):7252-67. doi: 10.1021/acs.jmedchem.6b00827. Epub 2016 Jul 25. J Med Chem. 2016. PMID: 27411843
Discovery of potent and specific CXCR3 antagonists.
Chen X, Mihalic J, Deignan J, Gustin DJ, Duquette J, Du X, Chan J, Fu Z, Johnson M, Li AR, Henne K, Sullivan T, Lemon B, Ma J, Miao S, Tonn G, Collins T, Medina JC. Chen X, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):357-62. doi: 10.1016/j.bmcl.2011.10.120. Epub 2011 Nov 9. Bioorg Med Chem Lett. 2012. PMID: 22130135
Discovery and in vivo evaluation of dual PI3Kβ/δ inhibitors.
Gonzalez-Lopez de Turiso F, Shin Y, Brown M, Cardozo M, Chen Y, Fong D, Hao X, He X, Henne K, Hu YL, Johnson MG, Kohn T, Lohman J, McBride HJ, McGee LR, Medina JC, Metz D, Miner K, Mohn D, Pattaropong V, Seganish J, Simard JL, Wannberg S, Whittington DA, Yu G, Cushing TD. Gonzalez-Lopez de Turiso F, et al. Among authors: johnson mg. J Med Chem. 2012 Sep 13;55(17):7667-85. doi: 10.1021/jm300679u. Epub 2012 Aug 29. J Med Chem. 2012. PMID: 22876881
Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
Cushing TD, Hao X, Shin Y, Andrews K, Brown M, Cardozo M, Chen Y, Duquette J, Fisher B, Gonzalez-Lopez de Turiso F, He X, Henne KR, Hu YL, Hungate R, Johnson MG, Kelly RC, Lucas B, McCarter JD, McGee LR, Medina JC, San Miguel T, Mohn D, Pattaropong V, Pettus LH, Reichelt A, Rzasa RM, Seganish J, Tasker AS, Wahl RC, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang D, Metz DP. Cushing TD, et al. Among authors: johnson mg. J Med Chem. 2015 Jan 8;58(1):480-511. doi: 10.1021/jm501624r. Epub 2014 Dec 3. J Med Chem. 2015. PMID: 25469863
Optimization of a series of quinazolinone-derived antagonists of CXCR3.
Liu J, Fu Z, Li AR, Johnson M, Zhu L, Marcus A, Danao J, Sullivan T, Tonn G, Collins T, Medina J. Liu J, et al. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5114-8. doi: 10.1016/j.bmcl.2009.07.032. Epub 2009 Jul 10. Bioorg Med Chem Lett. 2009. PMID: 19632842
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
Li AR, Johnson MG, Liu J, Chen X, Du X, Mihalic JT, Deignan J, Gustin DJ, Duquette J, Fu Z, Zhu L, Marcus AP, Bergeron P, McGee LR, Danao J, Lemon B, Carabeo T, Sullivan T, Ma J, Tang L, Tonn G, Collins TL, Medina JC. Li AR, et al. Among authors: johnson mg. Bioorg Med Chem Lett. 2008 Jan 15;18(2):688-93. doi: 10.1016/j.bmcl.2007.11.060. Epub 2007 Nov 21. Bioorg Med Chem Lett. 2008. PMID: 18061451
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
Kaizerman JA, Aaron W, An S, Austin R, Brown M, Chong A, Huang T, Hungate R, Jiang B, Johnson MG, Lee G, Lucas BS, Orf J, Rong M, Toteva MM, Wickramasinghe D, Xu G, Ye Q, Zhong W, McMinn DL. Kaizerman JA, et al. Among authors: johnson mg. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4607-10. doi: 10.1016/j.bmcl.2010.06.006. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20594845
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: johnson mg. 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
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
Liu J, Li AR, Wang Y, Johnson MG, Su Y, Shen W, Wang X, Lively S, Brown M, Lai S, Gonzalez Lopez De Turiso F, Xu Q, Van Lengerich B, Schmitt M, Fu Z, Sun Y, Lawlis S, Seitz L, Danao J, Wait J, Ye Q, Tang HL, Grillo M, Collins TL, Sullivan TJ, Medina JC. Liu J, et al. Among authors: johnson mg. ACS Med Chem Lett. 2011 Mar 2;2(5):326-30. doi: 10.1021/ml1002234. eCollection 2011 May 12. ACS Med Chem Lett. 2011. PMID: 24900313 Free PMC article.
407 results