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Highly selective c-Jun N-terminal kinase (JNK) 2 and 3 inhibitors with in vitro CNS-like pharmacokinetic properties prevent neurodegeneration.
Probst GD, Bowers S, Sealy JM, Truong AP, Hom RK, Galemmo RA Jr, Konradi AW, Sham HL, Quincy DA, Pan H, Yao N, Lin M, Tóth G, Artis DR, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura DF, Quinn KP, Sauer JM, Powell K, Ruslim L, Wright S, Chereau D, Ren Z, Anderson JP, Bard F, Yednock TA, Griswold-Prenner I. Probst GD, et al. Among authors: wong k. Bioorg Med Chem Lett. 2011 Jan 1;21(1):315-9. doi: 10.1016/j.bmcl.2010.11.010. Epub 2010 Nov 5. Bioorg Med Chem Lett. 2011. PMID: 21112785
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: wong k. 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
N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase.
Bowers S, Probst GD, Truong AP, Hom RK, Konradi AW, Sham HL, Garofalo AW, Wong K, Goldbach E, Quinn KP, Sauer JM, Wallace W, Nguyen L, Hemphill SS, Bova MP, Basi GS. Bowers S, et al. Among authors: wong k. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6952-6. doi: 10.1016/j.bmcl.2009.10.060. Epub 2009 Oct 30. Bioorg Med Chem Lett. 2009. PMID: 19879755
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.
Truong AP, Tóth G, Probst GD, Sealy JM, Bowers S, Wone DW, Dressen D, Hom RK, Konradi AW, Sham HL, Wu J, Peterson BT, Ruslim L, Bova MP, Kholodenko D, Motter RN, Bard F, Santiago P, Ni H, Chian D, Soriano F, Cole T, Brigham EF, Wong K, Zmolek W, Goldbach E, Samant B, Chen L, Zhang H, Nakamura DF, Quinn KP, Yednock TA, Sauer JM. Truong AP, et al. Among authors: wong k. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6231-6. doi: 10.1016/j.bmcl.2010.08.102. Epub 2010 Aug 24. Bioorg Med Chem Lett. 2010. PMID: 20833041
Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement.
Neitz RJ, Konradi AW, Sham HL, Zmolek W, Wong K, Qin A, Lorentzen C, Nakamura D, Quinn KP, Sauer JM, Powell K, Ruslim L, Chereau D, Ren Z, Anderson J, Bard F, Yednock TA, Griswold-Prenner I. Neitz RJ, et al. Among authors: wong k. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3726-9. doi: 10.1016/j.bmcl.2011.04.074. Epub 2011 Apr 27. Bioorg Med Chem Lett. 2011. PMID: 21570836
Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Bowers S, Truong AP, Jeffrey Neitz R, Hom RK, Sealy JM, Probst GD, Quincy D, Peterson B, Chan W, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Lin M, Yao N, Artis DR, Zhang H, Chen L, Dryer M, Samant B, Zmolek W, Wong K, Lorentzen C, Goldbach E, Tonn G, Quinn KP, Sauer JM, Wright S, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Bowers S, et al. Among authors: wong k. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5521-7. doi: 10.1016/j.bmcl.2011.06.100. Epub 2011 Jul 7. Bioorg Med Chem Lett. 2011. PMID: 21813278
Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors.
Aubele DL, Truong AP, Dressen DB, Probst GD, Bowers S, Mattson MN, Semko CM, Sun M, Garofalo AW, Konradi AW, Sham HL, Zmolek W, Wong K, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Nguyen L, Bova MP, Hemphill SS, Basi G. Aubele DL, et al. Among authors: wong k. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5791-4. doi: 10.1016/j.bmcl.2011.08.008. Epub 2011 Aug 9. Bioorg Med Chem Lett. 2011. PMID: 21885276
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: wong k. J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20. J Med Chem. 2013. PMID: 23713656
9,881 results