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SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H, Epshteyn S, Galan AA, Huynh TP, Ibrahim MA, Kane B, Koltun ES, Mann G, Meyr LE, Lee MS, Lewis GL, Noguchi RT, Pack M, Ridgway BH, Shi X, Takeuchi CS, Zu P, Leahy JW, Nuss JM, Aoyama R, Engst S, Gendreau SB, Kassees R, Li J, Lin SH, Martini JF, Stout T, Tong P, Woolfrey J, Zhang W, Yu P. Forsyth T, et al. Among authors: woolfrey j. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. doi: 10.1016/j.bmcl.2012.10.007. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23127890
Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists.
Ibrahim MA, Johnson HW, Jeong JW, Lewis GL, Shi X, Noguchi RT, Williams M, Leahy JW, Nuss JM, Woolfrey J, Banica M, Bentzien F, Chou YC, Gibson A, Heald N, Lamb P, Mattheakis L, Matthews D, Shipway A, Wu X, Zhang W, Zhou S, Shankar G. Ibrahim MA, et al. Among authors: woolfrey j. J Med Chem. 2012 Feb 9;55(3):1368-81. doi: 10.1021/jm201533b. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22214363
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Takeuchi CS, Kim BG, Blazey CM, Ma S, Johnson HW, Anand NK, Arcalas A, Baik TG, Buhr CA, Cannoy J, Epshteyn S, Joshi A, Lara K, Lee MS, Wang L, Leahy JW, Nuss JM, Aay N, Aoyama R, Foster P, Lee J, Lehoux I, Munagala N, Plonowski A, Rajan S, Woolfrey J, Yamaguchi K, Lamb P, Miller N. Takeuchi CS, et al. Among authors: woolfrey j. J Med Chem. 2013 Mar 28;56(6):2218-34. doi: 10.1021/jm3007933. Epub 2013 Mar 7. J Med Chem. 2013. PMID: 23394126
Parallel synthesis and structure-activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors.
Bauer SM, Goldman EA, Huang W, Su T, Wang L, Woolfrey J, Wu Y, Zuckett JF, Arfsten A, Huang B, Kothule J, Lin J, May B, Sinha U, Wong PW, Hutchaleelaha A, Scarborough RM, Zhu BY. Bauer SM, et al. Among authors: woolfrey j. Bioorg Med Chem Lett. 2004 Aug 2;14(15):4045-50. doi: 10.1016/j.bmcl.2004.05.033. Bioorg Med Chem Lett. 2004. PMID: 15225723
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.
Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY. Zhang P, et al. Among authors: woolfrey j. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85. doi: 10.1016/j.bmcl.2009.02.111. Epub 2009 Mar 3. Bioorg Med Chem Lett. 2009. PMID: 19297154
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.
Jia ZJ, Wu Y, Huang W, Zhang P, Song Y, Woolfrey J, Sinha U, Arfsten AE, Edwards ST, Hutchaleelaha A, Hollennbach SJ, Lambing JL, Scarborough RM, Zhu BY. Jia ZJ, et al. Among authors: woolfrey j. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1229-34. doi: 10.1016/j.bmcl.2003.12.054. Bioorg Med Chem Lett. 2004. PMID: 14980671
28 results