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Items: 18


Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase.

Selness SR, Boehm TL, Walker JK, Devadas B, Durley RC, Kurumbail R, Shieh H, Xing L, Hepperle M, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Devraj RV, Messing D, Schindler JF, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):4059-65. doi: 10.1016/j.bmcl.2011.04.120. Epub 2011 May 13.


Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase.

Jerome KD, Hepperle ME, Walker JK, Xing L, Devraj RV, Benson AG, Baldus JE, Selness SR.

Bioorg Med Chem Lett. 2010 May 15;20(10):3146-9. doi: 10.1016/j.bmcl.2010.03.088. Epub 2010 Mar 31.


Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase.

Walker JK, Selness SR, Devraj RV, Hepperle ME, Naing W, Shieh H, Kurambail R, Yang S, Flynn DL, Benson AG, Messing DM, Dice T, Kim T, Lindmark RJ, Monahan JB, Portanova J.

Bioorg Med Chem Lett. 2010 Apr 15;20(8):2634-8. doi: 10.1016/j.bmcl.2010.02.047. Epub 2010 Feb 14.


Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase.

Selness SR, Devraj RV, Monahan JB, Boehm TL, Walker JK, Devadas B, Durley RC, Kurumbail R, Shieh H, Xing L, Hepperle M, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R.

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5851-6. doi: 10.1016/j.bmcl.2009.08.082. Epub 2009 Aug 27.


Synthesis and antiviral activity of HCV NS3/4A peptidomimetic boronic acid inhibitors.

Boloor A, Hanway D, Joshi M, Winn DT, Mendez G, Walls M, Wei P, Qian F, Zhang X, Zhang Y, Hepperle ME, Li X, Campbell DA, Betancort JM.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5708-11. doi: 10.1016/j.bmcl.2009.08.017. Epub 2009 Aug 8.


SD0006: a potent, selective and orally available inhibitor of p38 kinase.

Burnette BL, Selness S, Devraj R, Jungbluth G, Kurumbail R, Stillwell L, Anderson G, Mnich S, Hirsch J, Compton R, De Ciechi P, Hope H, Hepperle M, Keith RH, Naing W, Shieh H, Portanova J, Zhang Y, Zhang J, Leimgruber RM, Monahan J.

Pharmacology. 2009;84(1):42-60. doi: 10.1159/000227286. Epub 2009 Jul 4.


Use of molecular imaging to quantify response to IKK-2 inhibitor treatment in murine arthritis.

Izmailova ES, Paz N, Alencar H, Chun M, Schopf L, Hepperle M, Lane JH, Harriman G, Xu Y, Ocain T, Weissleder R, Mahmood U, Healy AM, Jaffee B.

Arthritis Rheum. 2007 Jan;56(1):117-28.


IKKbeta inhibition protects against bone and cartilage destruction in a rat model of rheumatoid arthritis.

Schopf L, Savinainen A, Anderson K, Kujawa J, DuPont M, Silva M, Siebert E, Chandra S, Morgan J, Gangurde P, Wen D, Lane J, Xu Y, Hepperle M, Harriman G, Ocain T, Jaffee B.

Arthritis Rheum. 2006 Oct;54(10):3163-73.


A selective small molecule IkappaB Kinase beta inhibitor blocks nuclear factor kappaB-mediated inflammatory responses in human fibroblast-like synoviocytes, chondrocytes, and mast cells.

Wen D, Nong Y, Morgan JG, Gangurde P, Bielecki A, Dasilva J, Keaveney M, Cheng H, Fraser C, Schopf L, Hepperle M, Harriman G, Jaffee BD, Ocain TD, Xu Y.

J Pharmacol Exp Ther. 2006 Jun;317(3):989-1001. Epub 2006 Mar 8.


Rapid TNFR1-dependent lymphocyte depletion in vivo with a selective chemical inhibitor of IKKbeta.

Nagashima K, Sasseville VG, Wen D, Bielecki A, Yang H, Simpson C, Grant E, Hepperle M, Harriman G, Jaffee B, Ocain T, Xu Y, Fraser CC.

Blood. 2006 Jun 1;107(11):4266-73. Epub 2006 Jan 26.


Small molecule inhibitors of IkappaB kinase are selectively toxic for subgroups of diffuse large B-cell lymphoma defined by gene expression profiling.

Lam LT, Davis RE, Pierce J, Hepperle M, Xu Y, Hottelet M, Nong Y, Wen D, Adams J, Dang L, Staudt LM.

Clin Cancer Res. 2005 Jan 1;11(1):28-40.


The oxetane conformational lock of paclitaxel: structural analysis of D-secopaclitaxel.

Boge TC, Hepperle M, Vander Velde DG, Gunn CW, Grunewald GL, Georg GI.

Bioorg Med Chem Lett. 1999 Oct 18;9(20):3041-6.


Protection against beta-amyloid toxicity in primary neurons by paclitaxel (Taxol).

Michaelis ML, Ranciat N, Chen Y, Bechtel M, Ragan R, Hepperle M, Liu Y, Georg G.

J Neurochem. 1998 Apr;70(4):1623-7.


Probing the environment of tubulin-bound paclitaxel using fluorescent paclitaxel analogues.

Sengupta S, Boge TC, Liu Y, Hepperle M, Georg GI, Himes RH.

Biochemistry. 1997 Apr 29;36(17):5179-84.


Preparation of phenolic paclitaxel metabolites.

Park H, Hepperle M, Boge TC, Himes RH, Georg GI.

J Med Chem. 1996 Jul 5;39(14):2705-9.


Synthesis, Conformational Analysis, and Biological Evaluation of Heteroaromatic Taxanes.

Georg GI, Harriman GC, Hepperle M, Clowers JS, Vander Velde DG, Himes RH.

J Org Chem. 1996 Apr 19;61(8):2664-2676.


A research method to induce and examine a mild exacerbation of asthma by withdrawal of inhaled corticosteroid.

Gibson PG, Wong BJ, Hepperle MJ, Kline PA, Girgis-Gabardo A, Guyatt G, Dolovich J, Denburg JA, Ramsdale EH, Hargreave FE.

Clin Exp Allergy. 1992 May;22(5):525-32.


Airway hyperresponsiveness and asthma.

Hargreave FE, Gibson PG, Ramsdale EH, Fitzgerald JM, Hepperle MJ.

Agents Actions Suppl. 1989;28:205-11. Review. No abstract available.


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