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Items: 1 to 20 of 230

1.

Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.

Cheney IW, Yan S, Appleby T, Walker H, Vo T, Yao N, Hamatake R, Hong Z, Wu JZ.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83.

PMID:
17251021
2.

The discovery of novel benzofuran-2-carboxylic acids as potent Pim-1 inhibitors.

Xiang Y, Hirth B, Asmussen G, Biemann HP, Bishop KA, Good A, Fitzgerald M, Gladysheva T, Jain A, Jancsics K, Liu J, Metz M, Papoulis A, Skerlj R, Stepp JD, Wei RR.

Bioorg Med Chem Lett. 2011 May 15;21(10):3050-6. doi: 10.1016/j.bmcl.2011.03.030.

PMID:
21507633
3.

Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.

Tong Y, Stewart KD, Thomas S, Przytulinska M, Johnson EF, Klinghofer V, Leverson J, McCall O, Soni NB, Luo Y, Lin NH, Sowin TJ, Giranda VL, Penning TD.

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5206-8. doi: 10.1016/j.bmcl.2008.08.079.

PMID:
18790640
4.

A crystallographic fragment screen identifies cinnamic acid derivatives as starting points for potent Pim-1 inhibitors.

Schulz MN, Fanghänel J, Schäfer M, Badock V, Briem H, Boemer U, Nguyen D, Husemann M, Hillig RC.

Acta Crystallogr D Biol Crystallogr. 2011 Mar;67(Pt 3):156-66. doi: 10.1107/S0907444910054144.

PMID:
21358046
5.

A novel Pim-1 kinase inhibitor targeting residues that bind the substrate peptide.

Tsuganezawa K, Watanabe H, Parker L, Yuki H, Taruya S, Nakagawa Y, Kamei D, Mori M, Ogawa N, Tomabechi Y, Handa N, Honma T, Yokoyama S, Kojima H, Okabe T, Nagano T, Tanaka A.

J Mol Biol. 2012 Mar 30;417(3):240-52. doi: 10.1016/j.jmb.2012.01.036.

PMID:
22306408
6.

Structure-based design of 3-aryl-6-amino-triazolo[4,3-b]pyridazine inhibitors of Pim-1 kinase.

Grey R, Pierce AC, Bemis GW, Jacobs MD, Moody CS, Jajoo R, Mohal N, Green J.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3019-22. doi: 10.1016/j.bmcl.2009.04.061.

PMID:
19414255
7.

Comparative molecular field analysis of flavonoid inhibitors of the PIM-1 kinase.

Holder S, Lilly M, Brown ML.

Bioorg Med Chem. 2007 Oct 1;15(19):6463-73.

PMID:
17637507
8.

Small, low nanomolar, noncovalent thrombin inhibitors lacking a group to fill the 'distal binding pocket'.

Sanderson PE, Cutrona KJ, Dyer DL, Krueger JA, Kuo LC, Lewis SD, Lucas BJ, Yan Y.

Bioorg Med Chem Lett. 2003 Jan 20;13(2):161-4.

PMID:
12482415
9.

The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.

Cheung KM, Matthews TP, James K, Rowlands MG, Boxall KJ, Sharp SY, Maloney A, Roe SM, Prodromou C, Pearl LH, Aherne GW, McDonald E, Workman P.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3338-43.

PMID:
15955698
10.

Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase.

Pierce AC, Jacobs M, Stuver-Moody C.

J Med Chem. 2008 Mar 27;51(6):1972-5. doi: 10.1021/jm701248t.

PMID:
18290603
11.

Nonpeptidic inhibitors of human leukocyte elastase. 2. Design, synthesis, and in vitro activity of a series of 3-amino-6-arylopyridin-2-one trifluoromethyl ketones.

Damewood JR Jr, Edwards PD, Feeney S, Gomes BC, Steelman GB, Tuthill PA, Williams JC, Warner P, Woolson SA, Wolanin DJ, et al.

J Med Chem. 1994 Sep 30;37(20):3303-12.

PMID:
7932558
12.

Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase.

Holder S, Zemskova M, Zhang C, Tabrizizad M, Bremer R, Neidigh JW, Lilly MB.

Mol Cancer Ther. 2007 Jan;6(1):163-72.

13.

Non-peptidic inhibitors of human leukocyte elastase. 1. The design and synthesis of pyridone-containing inhibitors.

Warner P, Green RC, Gomes B, Strimpler AM.

J Med Chem. 1994 Sep 16;37(19):3090-9.

PMID:
7932532
14.

Hit to lead account of the discovery of a new class of inhibitors of Pim kinases and crystallographic studies revealing an unusual kinase binding mode.

Qian K, Wang L, Cywin CL, Farmer BT 2nd, Hickey E, Homon C, Jakes S, Kashem MA, Lee G, Leonard S, Li J, Magboo R, Mao W, Pack E, Peng C, Prokopowicz A 3rd, Welzel M, Wolak J, Morwick T.

J Med Chem. 2009 Apr 9;52(7):1814-27. doi: 10.1021/jm801242y.

PMID:
19256503
15.

Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.

Ala PJ, Gonneville L, Hillman M, Becker-Pasha M, Yue EW, Douty B, Wayland B, Polam P, Crawley ML, McLaughlin E, Sparks RB, Glass B, Takvorian A, Combs AP, Burn TC, Hollis GF, Wynn R.

J Biol Chem. 2006 Dec 8;281(49):38013-21.

16.

Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit.

Hu E, Tasker A, White RD, Kunz RK, Human J, Chen N, Bürli R, Hungate R, Novak P, Itano A, Zhang X, Yu V, Nguyen Y, Tudor Y, Plant M, Flynn S, Xu Y, Meagher KL, Whittington DA, Ng GY.

J Med Chem. 2008 Jun 12;51(11):3065-8. doi: 10.1021/jm800188g.

PMID:
18447379
17.

Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.

Sliman F, Blairvacq M, Durieu E, Meijer L, Rodrigo J, Desmaële D.

Bioorg Med Chem Lett. 2010 May 1;20(9):2801-5. doi: 10.1016/j.bmcl.2010.03.061.

PMID:
20363627
18.

A combination strategy to inhibit Pim-1: synergism between noncompetitive and ATP-competitive inhibitors.

Mori M, Tintori C, Christopher RS, Radi M, Schenone S, Musumeci F, Brullo C, Sanità P, Delle Monache S, Angelucci A, Kissova M, Crespan E, Maga G, Botta M.

ChemMedChem. 2013 Mar;8(3):484-96. doi: 10.1002/cmdc.201200480.

PMID:
23436791
19.

Identification of pyrrolo[2,3-g]indazoles as new Pim kinase inhibitors.

Gavara L, Suchaud V, Nauton L, Théry V, Anizon F, Moreau P.

Bioorg Med Chem Lett. 2013 Apr 15;23(8):2298-301. doi: 10.1016/j.bmcl.2013.02.074.

PMID:
23499503
20.

Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.

Liu M, Wang S, Clampit JE, Gum RJ, Haasch DL, Rondinone CM, Trevillyan JM, Abad-Zapatero C, Fry EH, Sham HL, Liu G.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):668-72.

PMID:
17107797

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