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Items: 1 to 50 of 125

1.

Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition.

Reich SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B, Ernst JT, Han Q, Goel VK, Han EZR, Huang V, Hung INJ, Jemison A, Jessen KA, Molter J, Murphy D, Neal M, Parker GS, Shaghafi M, Sperry S, Staunton J, Stumpf CR, Thompson PA, Tran C, Webber SE, Wegerski CJ, Zheng H, Webster KR.

J Med Chem. 2018 Apr 26;61(8):3516-3540. doi: 10.1021/acs.jmedchem.7b01795. Epub 2018 Mar 29.

PMID:
29526098
2.

Illuminator: increasing synergies between medicinal and computational chemists.

Gobbi A, Lardy M, Kim SH, Ruebsam F, Tran M, Webber SE, Xiang AX.

In Silico Biol. 2011-2012;11(1-2):83-93. doi: 10.3233/CI-2009-0017.

PMID:
22475753
3.

Discovery of tricyclic 5,6-dihydro-1H-pyridin-2-ones as novel, potent, and orally bioavailable inhibitors of HCV NS5B polymerase.

Ruebsam F, Murphy DE, Tran CV, Li LS, Zhao J, Dragovich PS, McGuire HM, Xiang AX, Sun Z, Ayida BK, Blazel JK, Kim SH, Zhou Y, Han Q, Kissinger CR, Webber SE, Showalter RE, Shah AM, Tsan M, Patel RA, Thompson PA, Lebrun LA, Hou HJ, Kamran R, Sergeeva MV, Bartkowski DM, Nolan TG, Norris DA, Khandurina J, Brooks J, Okamoto E, Kirkovsky L.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6404-12. doi: 10.1016/j.bmcl.2009.09.045. Epub 2009 Sep 17.

PMID:
19818610
4.

5,5'- and 6,6'-dialkyl-5,6-dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase.

Ellis DA, Blazel JK, Tran CV, Ruebsam F, Murphy DE, Li LS, Zhao J, Zhou Y, McGuire HM, Xiang AX, Webber SE, Zhao Q, Han Q, Kissinger CR, Lardy M, Gobbi A, Showalter RE, Shah AM, Tsan M, Patel RA, LeBrun LA, Kamran R, Bartkowski DM, Nolan TG, Norris DA, Sergeeva MV, Kirkovsky L.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6047-52. doi: 10.1016/j.bmcl.2009.09.051. Epub 2009 Sep 17.

PMID:
19796938
5.

5,6-Dihydro-1H-pyridin-2-ones as potent inhibitors of HCV NS5B polymerase.

Ruebsam F, Tran CV, Li LS, Kim SH, Xiang AX, Zhou Y, Blazel JK, Sun Z, Dragovich PS, Zhao J, McGuire HM, Murphy DE, Tran MT, Stankovic N, Ellis DA, Gobbi A, Showalter RE, Webber SE, Shah AM, Tsan M, Patel RA, Lebrun LA, Hou HJ, Kamran R, Sergeeva MV, Bartkowski DM, Nolan TG, Norris DA, Kirkovsky L.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):451-8. doi: 10.1016/j.bmcl.2008.11.048. Epub 2008 Nov 18.

PMID:
19054673
6.

Transcription inactivation through local refolding of the RNA polymerase structure.

Belogurov GA, Vassylyeva MN, Sevostyanova A, Appleman JR, Xiang AX, Lira R, Webber SE, Klyuyev S, Nudler E, Artsimovitch I, Vassylyev DG.

Nature. 2009 Jan 15;457(7227):332-5. doi: 10.1038/nature07510. Epub 2008 Oct 22.

7.

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 5: Exploration of pyridazinones containing 6-amino-substituents.

Dragovich PS, Blazel JK, Ellis DA, Han Q, Kamran R, Kissinger CR, LeBrun LA, Li LS, Murphy DE, Noble M, Patel RA, Ruebsam F, Sergeeva MV, Shah AM, Showalter RE, Tran CV, Tsan M, Webber SE, Kirkovsky L, Zhou Y.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5635-9. doi: 10.1016/j.bmcl.2008.08.094. Epub 2008 Aug 29.

PMID:
18796353
8.

Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.

Ruebsam F, Sun Z, Ayida BK, Webber SE, Zhou Y, Zhao Q, Kissinger CR, Showalter RE, Shah AM, Tsan M, Patel R, Lebrun LA, Kamran R, Sergeeva MV, Bartkowski DM, Nolan TG, Norris DA, Kirkovsky L.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5002-5. doi: 10.1016/j.bmcl.2008.08.017. Epub 2008 Aug 9.

PMID:
18722768
9.

4-(1,1-Dioxo-1,4-dihydro-1lambda6-benzo[1,4]thiazin-3-yl)-5-hydroxy-2H-pyridazin-3-ones as potent inhibitors of HCV NS5B polymerase.

Ellis DA, Blazel JK, Webber SE, Tran CV, Dragovich PS, Sun Z, Ruebsam F, McGuire HM, Xiang AX, Zhao J, Li LS, Zhou Y, Han Q, Kissinger CR, Showalter RE, Lardy M, Shah AM, Tsan M, Patel R, LeBrun LA, Kamran R, Bartkowski DM, Nolan TG, Norris DA, Sergeeva MV, Kirkovsky L.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4628-32. doi: 10.1016/j.bmcl.2008.07.014. Epub 2008 Jul 10.

PMID:
18662878
10.

Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase.

Kim SH, Tran MT, Ruebsam F, Xiang AX, Ayida B, McGuire H, Ellis D, Blazel J, Tran CV, Murphy DE, Webber SE, Zhou Y, Shah AM, Tsan M, Showalter RE, Patel R, Gobbi A, LeBrun LA, Bartkowski DM, Nolan TG, Norris DA, Sergeeva MV, Kirkovsky L, Zhao Q, Han Q, Kissinger CR.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4181-5. doi: 10.1016/j.bmcl.2008.05.083. Epub 2008 May 24.

PMID:
18554907
11.

Pyrrolo[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.

Ruebsam F, Webber SE, Tran MT, Tran CV, Murphy DE, Zhao J, Dragovich PS, Kim SH, Li LS, Zhou Y, Han Q, Kissinger CR, Showalter RE, Lardy M, Shah AM, Tsan M, Patel R, Lebrun LA, Kamran R, Sergeeva MV, Bartkowski DM, Nolan TG, Norris DA, Kirkovsky L.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3616-21. doi: 10.1016/j.bmcl.2008.04.066. Epub 2008 May 1.

PMID:
18487044
12.

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 3: Further optimization of the 2-, 6-, and 7'-substituents and initial pharmacokinetic assessments.

Li LS, Zhou Y, Murphy DE, Stankovic N, Zhao J, Dragovich PS, Bertolini T, Sun Z, Ayida B, Tran CV, Ruebsam F, Webber SE, Shah AM, Tsan M, Showalter RE, Patel R, Lebrun LA, Bartkowski DM, Nolan TG, Norris DA, Kamran R, Brooks J, Sergeeva MV, Kirkovsky L, Zhao Q, Kissinger CR.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3446-55. doi: 10.1016/j.bmcl.2008.02.072. Epub 2008 Mar 5.

PMID:
18457949
13.

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones: Part 4. Optimization of DMPK properties.

Sergeeva MV, Zhou Y, Bartkowski DM, Nolan TG, Norris DA, Okamoto E, Kirkovsky L, Kamran R, Lebrun LA, Tsan M, Patel R, Shah AM, Lardy M, Gobbi A, Li LS, Zhao J, Bertolini T, Stankovic N, Sun Z, Murphy DE, Webber SE, Dragovich PS.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3421-6. doi: 10.1016/j.bmcl.2008.04.005. Epub 2008 Apr 4.

PMID:
18442904
14.

Antibacterial activity in serum of the 3,5-diamino-piperidine translation inhibitors.

Zhou Y, Chow C, Murphy DE, Sun Z, Bertolini T, Froelich JM, Webber SE, Hermann T, Wall D.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3369-75. doi: 10.1016/j.bmcl.2008.04.023. Epub 2008 Apr 13.

15.

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 1: exploration of 7'-substitution of benzothiadiazine.

Zhou Y, Webber SE, Murphy DE, Li LS, Dragovich PS, Tran CV, Sun Z, Ruebsam F, Shah AM, Tsan M, Showalter RE, Patel R, Li B, Zhao Q, Han Q, Hermann T, Kissinger CR, Lebrun L, Sergeeva MV, Kirkovsky L.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1413-8. doi: 10.1016/j.bmcl.2008.01.007. Epub 2008 Jan 8.

PMID:
18242088
16.

Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 2: Variation of the 2- and 6-pyridazinone substituents.

Zhou Y, Li LS, Dragovich PS, Murphy DE, Tran CV, Ruebsam F, Webber SE, Shah AM, Tsan M, Averill A, Showalter RE, Patel R, Han Q, Zhao Q, Hermann T, Kissinger CR, Lebrun L, Sergeeva MV.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1419-24. doi: 10.1016/j.bmcl.2008.01.005. Epub 2008 Jan 8.

PMID:
18226901
17.

Discovery of ANA975: an oral prodrug of the TLR-7 agonist isatoribine.

Xiang AX, Webber SE, Kerr BM, Rueden EJ, Lennox JR, Haley GJ, Wang T, Ng JS, Herbert MR, Clark DL, Banh VN, Li W, Fletcher SP, Steffy KR, Bartkowski DM, Kirkovsky LI, Bauman LA, Averett DR.

Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):635-40.

PMID:
18066870
18.

Water-in-carbon dioxide emulsions stabilized with hydrophobic silica particles.

Adkins SS, Gohil D, Dickson JL, Webber SE, Johnston KP.

Phys Chem Chem Phys. 2007 Dec 28;9(48):6333-43. Epub 2007 Nov 8.

PMID:
18060163
19.

The pharmacology of endosomal TLR agonists in viral disease.

Averett DR, Fletcher SP, Li W, Webber SE, Appleman JR.

Biochem Soc Trans. 2007 Dec;35(Pt 6):1468-72. Review.

PMID:
18031247
20.

Syntheses of novel myxopyronin B analogs as potential inhibitors of bacterial RNA polymerase.

Lira R, Xiang AX, Doundoulakis T, Biller WT, Agrios KA, Simonsen KB, Webber SE, Sisson W, Aust RM, Shah AM, Showalter RE, Banh VN, Steffy KR, Appleman JR.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6797-800. Epub 2007 Oct 17.

PMID:
17980587
21.

Photophysics of water soluble perylene diimides in surfactant solutions.

Tang T, Peneva K, Müllen K, Webber SE.

J Phys Chem A. 2007 Oct 25;111(42):10609-14. Epub 2007 Oct 4.

PMID:
17915838
22.

Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial.

Thomas HD, Calabrese CR, Batey MA, Canan S, Hostomsky Z, Kyle S, Maegley KA, Newell DR, Skalitzky D, Wang LZ, Webber SE, Curtin NJ.

Mol Cancer Ther. 2007 Mar;6(3):945-56.

23.

Energy transfer in molecular layer-by-layer films of water-soluble perylene diimides.

Tang T, Herrmann A, Peneva K, Müllen K, Webber SE.

Langmuir. 2007 Apr 10;23(8):4623-8. Epub 2007 Mar 13.

PMID:
17352502
24.

Synthesis and SAR of 3,5-diamino-piperidine derivatives: novel antibacterial translation inhibitors as aminoglycoside mimetics.

Zhou Y, Gregor VE, Ayida BK, Winters GC, Sun Z, Murphy D, Haley G, Bailey D, Froelich JM, Fish S, Webber SE, Hermann T, Wall D.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1206-10. Epub 2006 Dec 12.

25.
26.
27.
28.

Deposition of cationic polymer micelles on planar SiO2 surfaces.

Hahn J, Webber SE.

Langmuir. 2004 May 11;20(10):4211-9.

PMID:
15969419
29.

Electrostatic stabilization of colloids in carbon dioxide: electrophoresis and dielectrophoresis.

Ryoo W, Dickson JL, Dhanuka VV, Webber SE, Bonnecaze RT, Johnston KP.

Langmuir. 2005 Jun 21;21(13):5914-23.

PMID:
15952842
30.

Preclinical profile of ciclesonide, a novel corticosteroid for the treatment of asthma.

Belvisi MG, Bundschuh DS, Stoeck M, Wicks S, Underwood S, Battram CH, Haddad el-B, Webber SE, Foster ML.

J Pharmacol Exp Ther. 2005 Aug;314(2):568-74. Epub 2005 May 5.

PMID:
15878996
31.

Graphoepitaxial deposition of cationic polymer micelles on patterned SiO2 surfaces.

Hahn J, Webber SE.

Langmuir. 2004 Feb 17;20(4):1489-94.

PMID:
15803739
32.

Myxopyronin B analogs as inhibitors of RNA polymerase, synthesis and biological evaluation.

Doundoulakis T, Xiang AX, Lira R, Agrios KA, Webber SE, Sisson W, Aust RM, Shah AM, Showalter RE, Appleman JR, Simonsen KB.

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5667-72.

PMID:
15482944
33.

Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.

Tikhe JG, Webber SE, Hostomsky Z, Maegley KA, Ekkers A, Li J, Yu XH, Almassy RJ, Kumpf RA, Boritzki TJ, Zhang C, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR.

J Med Chem. 2004 Oct 21;47(22):5467-81.

PMID:
15481984
34.

Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.

White AW, Curtin NJ, Eastman BW, Golding BT, Hostomsky Z, Kyle S, Li J, Maegley KA, Skalitzky DJ, Webber SE, Yu XH, Griffin RJ.

Bioorg Med Chem Lett. 2004 May 17;14(10):2433-7.

PMID:
15109627
35.

Novel poly(ADP-ribose) polymerase-1 inhibitor, AG14361, restores sensitivity to temozolomide in mismatch repair-deficient cells.

Curtin NJ, Wang LZ, Yiakouvaki A, Kyle S, Arris CA, Canan-Koch S, Webber SE, Durkacz BW, Calvert HA, Hostomsky Z, Newell DR.

Clin Cancer Res. 2004 Feb 1;10(3):881-9.

36.

Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361.

Calabrese CR, Almassy R, Barton S, Batey MA, Calvert AH, Canan-Koch S, Durkacz BW, Hostomsky Z, Kumpf RA, Kyle S, Li J, Maegley K, Newell DR, Notarianni E, Stratford IJ, Skalitzky D, Thomas HD, Wang LZ, Webber SE, Williams KJ, Curtin NJ.

J Natl Cancer Inst. 2004 Jan 7;96(1):56-67.

PMID:
14709739
37.

Carbon dioxide-in-water microemulsions.

Lee CT Jr, Ryoo W, Smith PG Jr, Arellano J, Mitchell DR, Lagow RJ, Webber SE, Johnston KP.

J Am Chem Soc. 2003 Mar 12;125(10):3181-9. Erratum in: J Am Chem Soc. 2003 Dec 10;125(49):15268.

PMID:
12617686
38.

Pharmacological assessment of the nitric-oxide synthase isoform involved in eosinophilic inflammation in a rat model of sephadex-induced airway inflammation.

Birrell MA, McCluskie K, Haddad el-B, Battram CH, Webber SE, Foster ML, Yacoub MH, Belvisi MG.

J Pharmacol Exp Ther. 2003 Mar;304(3):1285-91.

PMID:
12604708
39.

Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.

Skalitzky DJ, Marakovits JT, Maegley KA, Ekker A, Yu XH, Hostomsky Z, Webber SE, Eastman BW, Almassy R, Li J, Curtin NJ, Newell DR, Calvert AH, Griffin RJ, Golding BT.

J Med Chem. 2003 Jan 16;46(2):210-3.

PMID:
12519059
40.

Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.

Canan Koch SS, Thoresen LH, Tikhe JG, Maegley KA, Almassy RJ, Li J, Yu XH, Zook SE, Kumpf RA, Zhang C, Boritzki TJ, Mansour RN, Zhang KE, Ekker A, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR, Webber SE, Hostomsky Z.

J Med Chem. 2002 Nov 7;45(23):4961-74.

PMID:
12408707
41.

Functional characterization and biomarker identification in the Brown Norway model of allergic airway inflammation.

Underwood SL, Haddad el-B, Birrell MA, McCluskie K, Pecoraro M, Dabrowski D, Webber SE, Foster ML, Belvisi MG.

Br J Pharmacol. 2002 Sep;137(2):263-75.

42.

Differential effects of ebselen on neutrophil recruitment, chemokine, and inflammatory mediator expression in a rat model of lipopolysaccharide-induced pulmonary inflammation.

Haddad el-B, McCluskie K, Birrell MA, Dabrowski D, Pecoraro M, Underwood S, Chen B, De Sanctis GT, Webber SE, Foster ML, Belvisi MG.

J Immunol. 2002 Jul 15;169(2):974-82.

43.

Hand-held three-dimensional dental X-ray system: technical description and preliminary results.

Webber RL, Webber SE, Moore J.

Dentomaxillofac Radiol. 2002 Jul;31(4):240-8.

PMID:
12087441
44.

Design and synthesis of irreversible depsipeptidyl human rhinovirus 3C protease inhibitors.

Webber SE, Marakovits JT, Dragovich PS, Prins TJ, Zhou R, Fuhrman SA, Patick AK, Matthews DA, Lee CA, Srinivasan B, Moran T, Ford CE, Brothers MA, Harr JE, Meador JW 3rd, Ferre RA, Worland ST.

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2683-6.

PMID:
11591501
45.

Role of p38 MAP kinase in LPS-induced airway inflammation in the rat.

Haddad EB, Birrell M, McCluskie K, Ling A, Webber SE, Foster ML, Belvisi MG.

Br J Pharmacol. 2001 Apr;132(8):1715-24.

46.

Therapeutic benefit of a dissociated glucocorticoid and the relevance of in vitro separation of transrepression from transactivation activity.

Belvisi MG, Wicks SL, Battram CH, Bottoms SE, Redford JE, Woodman P, Brown TJ, Webber SE, Foster ML.

J Immunol. 2001 Feb 1;166(3):1975-82.

47.
49.

Effect of the p38 kinase inhibitor, SB 203580, on allergic airway inflammation in the rat.

Escott KJ, Belvisi MG, Birrell MA, Webber SE, Foster ML, Sargent CA.

Br J Pharmacol. 2000 Sep;131(2):173-6.

50.

Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors.

Dragovich PS, Zhou R, Webber SE, Prins TJ, Kwok AK, Okano K, Fuhrman SA, Zalman LS, Maldonado FC, Brown EL, Meador JW 3rd, Patick AK, Ford CE, Brothers MA, Binford SL, Matthews DA, Ferre RA, Worland ST.

Bioorg Med Chem Lett. 2000 Jan 3;10(1):45-8.

PMID:
10636240

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