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Items: 16

1.

Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.

Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Jones GE, Kusalakumari Sukmar SK, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND.

Bioorg Med Chem Lett. 2016 May 15;26(10):2464-2469. doi: 10.1016/j.bmcl.2016.03.106. Epub 2016 Mar 31.

PMID:
27055939
2.

Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor.

Dumble M, Crouthamel MC, Zhang SY, Schaber M, Levy D, Robell K, Liu Q, Figueroa DJ, Minthorn EA, Seefeld MA, Rouse MB, Rabindran SK, Heerding DA, Kumar R.

PLoS One. 2014 Jun 30;9(6):e100880. doi: 10.1371/journal.pone.0100880. eCollection 2014.

3.

Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.

Miles TJ, Hennessy AJ, Bax B, Brooks G, Brown BS, Brown P, Cailleau N, Chen D, Dabbs S, Davies DT, Esken JM, Giordano I, Hoover JL, Huang J, Jones GE, Sukmar SK, Spitzfaden C, Markwell RE, Minthorn EA, Rittenhouse S, Gwynn MN, Pearson ND.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5437-41. doi: 10.1016/j.bmcl.2013.07.013. Epub 2013 Jul 17.

PMID:
23968823
4.

Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.

Miles TJ, Axten JM, Barfoot C, Brooks G, Brown P, Chen D, Dabbs S, Davies DT, Downie DL, Eyrisch S, Gallagher T, Giordano I, Gwynn MN, Hennessy A, Hoover J, Huang J, Jones G, Markwell R, Miller WH, Minthorn EA, Rittenhouse S, Seefeld M, Pearson N.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7489-95. doi: 10.1016/j.bmcl.2011.09.117. Epub 2011 Oct 10.

PMID:
22047689
5.

Pharmacokinetics and pharmacodynamics of mepolizumab, an anti-interleukin-5 monoclonal antibody.

Smith DA, Minthorn EA, Beerahee M.

Clin Pharmacokinet. 2011 Apr;50(4):215-27. doi: 10.2165/11584340-000000000-00000. Review.

PMID:
21348536
6.

GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition.

Gilmartin AG, Bleam MR, Groy A, Moss KG, Minthorn EA, Kulkarni SG, Rominger CM, Erskine S, Fisher KE, Yang J, Zappacosta F, Annan R, Sutton D, Laquerre SG.

Clin Cancer Res. 2011 Mar 1;17(5):989-1000. doi: 10.1158/1078-0432.CCR-10-2200. Epub 2011 Jan 18. Erratum in: Clin Cancer Res. 2012 Apr 15;18(8):2413.

7.

Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.

Lin H, Yamashita DS, Xie R, Zeng J, Wang W, Leber J, Safonov IG, Verma S, Li M, Lafrance L, Venslavsky J, Takata D, Luengo JI, Kahana JA, Zhang S, Robell KA, Levy D, Kumar R, Choudhry AE, Schaber M, Lai Z, Brown BS, Donovan BT, Minthorn EA, Brown KK, Heerding DA.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):684-8. doi: 10.1016/j.bmcl.2009.11.061. Epub 2009 Dec 16.

PMID:
20006500
8.

2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.

Lin H, Yamashita DS, Zeng J, Xie R, Wang W, Nidarmarthy S, Luengo JI, Rhodes N, Knick VB, Choudhry AE, Lai Z, Minthorn EA, Strum SL, Wood ER, Elkins PA, Concha NO, Heerding DA.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):673-8. doi: 10.1016/j.bmcl.2009.11.064. Epub 2009 Nov 20.

PMID:
20006497
9.

2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.

Lin H, Yamashita DS, Zeng J, Xie R, Verma S, Luengo JI, Rhodes N, Zhang S, Robell KA, Choudhry AE, Lai Z, Kumar R, Minthorn EA, Brown KK, Heerding DA.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83. doi: 10.1016/j.bmcl.2009.11.060. Epub 2009 Nov 20.

PMID:
20005102
10.

Discovery of 5-pyrrolopyridinyl-2-thiophenecarboxamides as potent AKT kinase inhibitors.

Seefeld MA, Rouse MB, McNulty KC, Sun L, Wang J, Yamashita DS, Luengo JI, Zhang S, Minthorn EA, Concha NO, Heerding DA.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2244-8. doi: 10.1016/j.bmcl.2009.02.094. Epub 2009 Feb 27.

PMID:
19285393
11.

Aminofurazans as potent inhibitors of AKT kinase.

Rouse MB, Seefeld MA, Leber JD, McNulty KC, Sun L, Miller WH, Zhang S, Minthorn EA, Concha NO, Choudhry AE, Schaber MD, Heerding DA.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1508-11. doi: 10.1016/j.bmcl.2009.01.002. Epub 2009 Jan 9.

PMID:
19179070
12.

Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.

Heerding DA, Rhodes N, Leber JD, Clark TJ, Keenan RM, Lafrance LV, Li M, Safonov IG, Takata DT, Venslavsky JW, Yamashita DS, Choudhry AE, Copeland RA, Lai Z, Schaber MD, Tummino PJ, Strum SL, Wood ER, Duckett DR, Eberwein D, Knick VB, Lansing TJ, McConnell RT, Zhang S, Minthorn EA, Concha NO, Warren GL, Kumar R.

J Med Chem. 2008 Sep 25;51(18):5663-79. doi: 10.1021/jm8004527.

PMID:
18800763
13.

Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity.

Rhodes N, Heerding DA, Duckett DR, Eberwein DJ, Knick VB, Lansing TJ, McConnell RT, Gilmer TM, Zhang SY, Robell K, Kahana JA, Geske RS, Kleymenova EV, Choudhry AE, Lai Z, Leber JD, Minthorn EA, Strum SL, Wood ER, Huang PS, Copeland RA, Kumar R.

Cancer Res. 2008 Apr 1;68(7):2366-74. doi: 10.1158/0008-5472.CAN-07-5783.

14.

Pharmacokinetic and pharmacodynamic modeling of humanized anti-factor IX antibody (SB 249417) in humans.

Chow FS, Benincosa LJ, Sheth SB, Wilson D, Davis CB, Minthorn EA, Jusko WJ.

Clin Pharmacol Ther. 2002 Apr;71(4):235-45.

PMID:
11956506
15.

A population pharmacokinetic-pharmacodynamic analysis of single doses of clenoliximab in patients with rheumatoid arthritis.

Mould DR, Davis CB, Minthorn EA, Kwok DC, Elliott MJ, Luggen ME, Totoritis MC.

Clin Pharmacol Ther. 1999 Sep;66(3):246-57.

PMID:
10511060
16.

The pharmacokinetics of topotecan and its carboxylate form following separate intravenous administration to the dog.

Davies BE, Minthorn EA, Dennis MJ, Rosing H, Beijnen JH.

Pharm Res. 1997 Oct;14(10):1461-5.

PMID:
9358562

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