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Page 1
Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.
Cee VJ, Chavez F Jr, Herberich B, Lanman BA, Pettus LH, Reed AB, Wu B, Wurz RP, Andrews KL, Chen J, Hickman D, Laszlo J 3rd, Lee MR, Guerrero N, Mattson BK, Nguyen Y, Mohr C, Rex K, Sastri CE, Wang P, Wu Q, Wu T, Xu Y, Zhou Y, Winston JT, Lipford JR, Tasker AS, Wang HL. Cee VJ, et al. Among authors: tasker as. ACS Med Chem Lett. 2016 Feb 12;7(4):408-12. doi: 10.1021/acsmedchemlett.5b00403. eCollection 2016 Apr 14. ACS Med Chem Lett. 2016. PMID: 27096050 Free PMC article.
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
Norman MH, Andrews KL, Bo YY, Booker SK, Caenepeel S, Cee VJ, D'Angelo ND, Freeman DJ, Herberich BJ, Hong FT, Jackson CL, Jiang J, Lanman BA, Liu L, McCarter JD, Mullady EL, Nishimura N, Pettus LH, Reed AB, Miguel TS, Smith AL, Stec MM, Tadesse S, Tasker A, Aidasani D, Zhu X, Subramanian R, Tamayo NA, Wang L, Whittington DA, Wu B, Wu T, Wurz RP, Yang K, Zalameda L, Zhang N, Hughes PE. Norman MH, et al. J Med Chem. 2012 Sep 13;55(17):7796-816. doi: 10.1021/jm300846z. Epub 2012 Aug 30. J Med Chem. 2012. PMID: 22897589
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. 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.
Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Wurz RP, Pettus LH, Henkle B, Sherman L, Plant M, Miner K, McBride HJ, Wong LM, Saris CJ, Lee MR, Chmait S, Mohr C, Hsieh F, Tasker AS. Wurz RP, et al. Among authors: tasker as. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1680-4. doi: 10.1016/j.bmcl.2010.01.059. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20138761
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
Pettus LH, Wurz RP, Xu S, Herberich B, Henkle B, Liu Q, McBride HJ, Mu S, Plant MH, Saris CJ, Sherman L, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS. Pettus LH, et al. Among authors: tasker as. J Med Chem. 2010 Apr 8;53(7):2973-85. doi: 10.1021/jm100095x. J Med Chem. 2010. PMID: 20218619
Identification of triazolopyridazinones as potent p38α inhibitors.
Herberich B, Jackson C, Wurz RP, Pettus LH, Sherman L, Liu Q, Henkle B, Saris CJ, Wong LM, Chmait S, Lee MR, Mohr C, Hsieh F, Tasker AS. Herberich B, et al. Among authors: tasker as. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1226-9. doi: 10.1016/j.bmcl.2011.11.067. Epub 2011 Nov 23. Bioorg Med Chem Lett. 2012. PMID: 22196117
Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511.
Lanman BA, Reed AB, Cee VJ, Hong FT, Pettus LH, Wurz RP, Andrews KL, Jiang J, McCarter JD, Mullady EL, San Miguel T, Subramanian R, Wang L, Whittington DA, Wu T, Zalameda L, Zhang N, Tasker AS, Hughes PE, Norman MH. Lanman BA, et al. Among authors: tasker as. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5630-5634. doi: 10.1016/j.bmcl.2014.10.085. Epub 2014 Nov 1. Bioorg Med Chem Lett. 2014. PMID: 25466188
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: tasker as. 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
The discovery and optimization of aminooxadiazoles as potent Pim kinase inhibitors.
Wurz RP, Pettus LH, Jackson C, Wu B, Wang HL, Herberich B, Cee V, Lanman BA, Reed AB, Chavez F Jr, Nixey T, Laszlo J 3rd, Wang P, Nguyen Y, Sastri C, Guerrero N, Winston J, Lipford JR, Lee MR, Andrews KL, Mohr C, Xu Y, Zhou Y, Reid DL, Tasker AS. Wurz RP, et al. Among authors: tasker as. Bioorg Med Chem Lett. 2015 Feb 15;25(4):847-55. doi: 10.1016/j.bmcl.2014.12.067. Epub 2015 Jan 7. Bioorg Med Chem Lett. 2015. PMID: 25599837
52 results