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Page 1
Arylsulfonamide pyrimidines as VLA-4 antagonists.
Xu YZ, Konradi AW, Bard F, Dappen M, Dofiles L, Dreyer M, Gallager I, Garrido C, Krimm M, Liao Z, Messersmith E, Mutter L, Pleiss MA, Samant B, Semko CM, Smith J, Stappenbeck F, Stupi B, Vandervert C, Welch B, Wipke B, Yednock T. Xu YZ, et al. Among authors: dappen m. Bioorg Med Chem Lett. 2013 May 15;23(10):3070-4. doi: 10.1016/j.bmcl.2013.03.010. Epub 2013 Mar 15. Bioorg Med Chem Lett. 2013. PMID: 23562062
PEG conjugates of potent α4 integrin inhibitors, maintaining sustained levels and bioactivity in vivo, following subcutaneous administration.
Smith JL, Rossiter KI, Semko CM, Xu YZ, Quincy DA, Jagodzinski J, Dappen MS, Konradi AW, Vandevert C, Garrido C, Mao W, San Pablo FB, Wipke B, Dofiles L, Wadsworth A, Peterson E, Lorenzana C, Simmonds S, Messersmith EK, Bard F, Pleiss MA, Yednock TA. Smith JL, et al. Among authors: dappen ms. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4117-9. doi: 10.1016/j.bmcl.2013.05.048. Epub 2013 May 24. Bioorg Med Chem Lett. 2013. PMID: 23743283
Orally available and efficacious α4β1/α4β7 integrin inhibitors.
Xu YZ, Smith JL, Semko CM, Rossiter KI, Fukuda JY, Dappen MS, Quincy DA, Konradi AW, Mao W, Welch B, Dreyer ML, Samant B, Zhang H, Lugar J, Liao Z, Henschel C, Petersen E, Vandevert C, Shoemaker M, Wehner N, Mutter L, Shopp G, Krimm M, Chen L, Wipke B, Dofiles L, Gallager I, Sauer JM, Messersmith EK, Pleiss MA, Bard F, Yednock TA. Xu YZ, et al. Among authors: dappen ms. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4370-3. doi: 10.1016/j.bmcl.2013.05.076. Epub 2013 May 31. Bioorg Med Chem Lett. 2013. PMID: 23777782
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.
Ng RA, Sun M, Bowers S, Hom RK, Probst GD, John V, Fang LY, Maillard M, Gailunas A, Brogley L, Neitz RJ, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Adler M, Yao N, Zmolek W, Nakamura D, Quinn KP, Sauer JM, Bova MP, Ruslim L, Artis DR, Yednock TA. Ng RA, et al. Among authors: dappen ms. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4674-9. doi: 10.1016/j.bmcl.2013.06.006. Epub 2013 Jun 11. Bioorg Med Chem Lett. 2013. PMID: 23856050
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
Ye XM, Konradi AW, Sun M, Yuan S, Aubele DL, Dappen M, Dressen D, Garofalo AW, Jagodzinski JJ, Latimer L, Probst GD, Sham HL, Wone D, Xu YZ, Ness D, Brigham E, Kwong GT, Willtis C, Tonn G, Goldbach E, Quinn KP, Zhang HH, Sauer JM, Bova M, Basi GS. Ye XM, et al. Among authors: dappen m. Bioorg Med Chem Lett. 2013 Feb 15;23(4):996-1000. doi: 10.1016/j.bmcl.2012.12.039. Epub 2012 Dec 21. Bioorg Med Chem Lett. 2013. PMID: 23312944
Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
Truong AP, Aubele DL, Probst GD, Neitzel ML, Semko CM, Bowers S, Dressen D, Hom RK, Konradi AW, Sham HL, Garofalo AW, Keim PS, Wu J, Dappen MS, Wong K, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Nguyen L, Hemphill SS, Bova MP, Bard F, Yednock TA, Basi G. Truong AP, et al. Among authors: dappen ms. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4920-3. doi: 10.1016/j.bmcl.2009.07.092. Epub 2009 Jul 23. Bioorg Med Chem Lett. 2009. PMID: 19660943
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.
Sealy JM, Truong AP, Tso L, Probst GD, Aquino J, Hom RK, Jagodzinska BM, Dressen D, Wone DW, Brogley L, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Dappen MS, Toth G, Pan H, Ruslim L, Miller J, Bova MP, Sinha S, Quinn KP, Sauer JM. Sealy JM, et al. Among authors: dappen ms. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6386-91. doi: 10.1016/j.bmcl.2009.09.061. Epub 2009 Sep 19. Bioorg Med Chem Lett. 2009. PMID: 19811916
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.
Truong AP, Probst GD, Aquino J, Fang L, Brogley L, Sealy JM, Hom RK, Tucker JA, John V, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Tóth G, Yao N, Brecht E, Pan H, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Zmolek W, Quinn KP, Sauer JM. Truong AP, et al. Among authors: dappen ms. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4789-94. doi: 10.1016/j.bmcl.2010.06.112. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20634069
Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.
Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA Jr, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Pandya D, Diep L, Fitzgerald K, Artis DR, Anderson JP, Bergeron M. Bowers S, et al. Among authors: dappen ms. Bioorg Med Chem Lett. 2013 May 1;23(9):2743-9. doi: 10.1016/j.bmcl.2013.02.065. Epub 2013 Feb 24. Bioorg Med Chem Lett. 2013. PMID: 23522834
Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.
Probst G, Aubele DL, Bowers S, Dressen D, Garofalo AW, Hom RK, Konradi AW, Marugg JL, Mattson MN, Neitzel ML, Semko CM, Sham HL, Smith J, Sun M, Truong AP, Ye XM, Xu YZ, Dappen MS, Jagodzinski JJ, Keim PS, Peterson B, Latimer LH, Quincy D, Wu J, Goldbach E, Ness DK, Quinn KP, Sauer JM, Wong K, Zhang H, Zmolek W, Brigham EF, Kholodenko D, Hu K, Kwong GT, Lee M, Liao A, Motter RN, Sacayon P, Santiago P, Willits C, Bard F, Bova MP, Hemphill SS, Nguyen L, Ruslim L, Tanaka K, Tanaka P, Wallace W, Yednock TA, Basi GS. Probst G, et al. Among authors: dappen ms. J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20. J Med Chem. 2013. PMID: 23713656
23 results