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Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
Skoumbourdis AP, Leclair CA, Stefan E, Turjanski AG, Maguire W, Titus SA, Huang R, Auld DS, Inglese J, Austin CP, Michnick SW, Xia M, Thomas CJ. Skoumbourdis AP, et al. Among authors: austin cp. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3686-92. doi: 10.1016/j.bmcl.2009.01.057. Epub 2009 Jan 23. Bioorg Med Chem Lett. 2009. PMID: 19464886 Free PMC article.
N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.
Huang W, Zheng W, Urban DJ, Inglese J, Sidransky E, Austin CP, Thomas CJ. Huang W, et al. Among authors: austin cp. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5783-9. doi: 10.1016/j.bmcl.2007.08.050. Epub 2007 Aug 28. Bioorg Med Chem Lett. 2007. PMID: 17827006 Free PMC article.
Identification of a potent new chemotype for the selective inhibition of PDE4.
Skoumbourdis AP, Huang R, Southall N, Leister W, Guo V, Cho MH, Inglese J, Nirenberg M, Austin CP, Xia M, Thomas CJ. Skoumbourdis AP, et al. Among authors: austin cp. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1297-303. doi: 10.1016/j.bmcl.2008.01.028. Epub 2008 Jan 11. Bioorg Med Chem Lett. 2008. PMID: 18243697 Free PMC article.
Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Jiang JK, Boxer MB, Vander Heiden MG, Shen M, Skoumbourdis AP, Southall N, Veith H, Leister W, Austin CP, Park HW, Inglese J, Cantley LC, Auld DS, Thomas CJ. Jiang JK, et al. Among authors: austin cp. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3387-93. doi: 10.1016/j.bmcl.2010.04.015. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20451379 Free PMC article.
Fluorescence spectroscopic profiling of compound libraries.
Simeonov A, Jadhav A, Thomas CJ, Wang Y, Huang R, Southall NT, Shinn P, Smith J, Austin CP, Auld DS, Inglese J. Simeonov A, et al. Among authors: austin cp. J Med Chem. 2008 Apr 24;51(8):2363-71. doi: 10.1021/jm701301m. Epub 2008 Mar 26. J Med Chem. 2008. PMID: 18363325
271 results