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Items: 1 to 20 of 227

1.

Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator.

Frederickson M, Callaghan O, Chessari G, Congreve M, Cowan SR, Matthews JE, McMenamin R, Smith DM, Vinković M, Wallis NG.

J Med Chem. 2008 Jan 24;51(2):183-6. doi: 10.1021/jm701359z. Epub 2007 Dec 29.

PMID:
18163548
2.

Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA).

West CW, Adler M, Arnaiz D, Chen D, Chu K, Gualtieri G, Ho E, Huwe C, Light D, Phillips G, Pulk R, Sukovich D, Whitlow M, Yuan S, Bryant J.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5712-5. doi: 10.1016/j.bmcl.2009.08.008. Epub 2009 Aug 7.

PMID:
19703768
3.

2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

Mackman RL, Hui HC, Breitenbucher JG, Katz BA, Luong C, Martelli A, McGee D, Radika K, Sendzik M, Spencer JR, Sprengeler PA, Tario J, Verner E, Wang J.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2019-22.

PMID:
12113832
4.

(4-aminomethyl)phenylguanidine derivatives as nonpeptidic highly selective inhibitors of human urokinase.

Sperl S, Jacob U, Arroyo de Prada N, Stürzebecher J, Wilhelm OG, Bode W, Magdolen V, Huber R, Moroder L.

Proc Natl Acad Sci U S A. 2000 May 9;97(10):5113-8.

5.

Design of novel and selective inhibitors of urokinase-type plasminogen activator with improved pharmacokinetic properties for use as antimetastatic agents.

Schweinitz A, Steinmetzer T, Banke IJ, Arlt MJ, Stürzebecher A, Schuster O, Geissler A, Giersiefen H, Zeslawska E, Jacob U, Krüger A, Stürzebecher J.

J Biol Chem. 2004 Aug 6;279(32):33613-22. Epub 2004 May 18.

6.

Crystals of urokinase type plasminogen activator complexes reveal the binding mode of peptidomimetic inhibitors.

Zeslawska E, Jacob U, Schweinitz A, Coombs G, Bode W, Madison E.

J Mol Biol. 2003 Apr 18;328(1):109-18.

PMID:
12684001
7.

4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

Spencer JR, McGee D, Allen D, Katz BA, Luong C, Sendzik M, Squires N, Mackman RL.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2023-6.

PMID:
12113833
8.

Inhibitors of the protease domain of urokinase-type plasminogen activator.

Rockway TW, Nienaber V, Giranda VL.

Curr Pharm Des. 2002;8(28):2541-58. Review.

PMID:
12369939
9.

Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.

Joossens J, Van der Veken P, Surpateanu G, Lambeir AM, El-Sayed I, Ali OM, Augustyns K, Haemers A.

J Med Chem. 2006 Sep 21;49(19):5785-93.

PMID:
16970403
10.

Structure-directed discovery of potent non-peptidic inhibitors of human urokinase that access a novel binding subsite.

Nienaber VL, Davidson D, Edalji R, Giranda VL, Klinghofer V, Henkin J, Magdalinos P, Mantei R, Merrick S, Severin JM, Smith RA, Stewart K, Walter K, Wang J, Wendt M, Weitzberg M, Zhao X, Rockway T.

Structure. 2000 May 15;8(5):553-63.

11.

Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.

Mackman RL, Katz BA, Breitenbucher JG, Hui HC, Verner E, Luong C, Liu L, Sprengeler PA.

J Med Chem. 2001 Nov 8;44(23):3856-71.

PMID:
11689072
12.

Identification of novel inhibitors of urokinase via NMR-based screening.

Hajduk PJ, Boyd S, Nettesheim D, Nienaber V, Severin J, Smith R, Davidson D, Rockway T, Fesik SW.

J Med Chem. 2000 Oct 19;43(21):3862-6.

PMID:
11052791
13.

Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines.

Fish PV, Barber CG, Brown DG, Butt R, Collis MG, Dickinson RP, Henry BT, Horne VA, Huggins JP, King E, O'Gara M, McCleverty D, McIntosh F, Phillips C, Webster R.

J Med Chem. 2007 May 17;50(10):2341-51. Epub 2007 Apr 21.

PMID:
17447747
14.

Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone.

Kung PP, Huang B, Zhang G, Zhou JZ, Wang J, Digits JA, Skaptason J, Yamazaki S, Neul D, Zientek M, Elleraas J, Mehta P, Yin MJ, Hickey MJ, Gajiwala KS, Rodgers C, Davies JF, Gehring MR.

J Med Chem. 2010 Jan 14;53(1):499-503. doi: 10.1021/jm901209q.

PMID:
19908836
15.

Discovering novel ligands for macromolecules using X-ray crystallographic screening.

Nienaber VL, Richardson PL, Klighofer V, Bouska JJ, Giranda VL, Greer J.

Nat Biotechnol. 2000 Oct;18(10):1105-8.

PMID:
11017052
16.

Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.

Wendt MD, Rockway TW, Geyer A, McClellan W, Weitzberg M, Zhao X, Mantei R, Nienaber VL, Stewart K, Klinghofer V, Giranda VL.

J Med Chem. 2004 Jan 15;47(2):303-24.

PMID:
14711304
17.

Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.

Barber CG, Dickinson RP, Horne VA.

Bioorg Med Chem Lett. 2002 Jan 21;12(2):181-4.

PMID:
11755349
18.

Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).

Katz BA, Luong C, Ho JD, Somoza JR, Gjerstad E, Tang J, Williams SR, Verner E, Mackman RL, Young WB, Sprengeler PA, Chan H, Mortara K, Janc JW, McGrath ME.

J Mol Biol. 2004 Nov 19;344(2):527-47.

PMID:
15522303
19.

The crystal structures of 3-TAPAP in complexes with the urokinase-type plasminogen activator and picrate.

Zesławska E, Jacob U, Stürzebecher J, Oleksyn BJ.

Bioorg Med Chem Lett. 2006 Jan 1;16(1):228-34. Epub 2005 Oct 3.

PMID:
16202591
20.

Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.

Subasinghe NL, Illig C, Hoffman J, Rudolph MJ, Wilson KJ, Soll R, Randle T, Green D, Lewandowski F, Zhang M, Bone R, Spurlino J, DesJarlais R, Deckman I, Molloy CJ, Manthey C, Zhou Z, Sharp C, Maguire D, Crysler C, Grasberger B.

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1379-82.

PMID:
11378359
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