BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

214 related articles for article (PubMed ID: 16821787)

  • 1. Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human beta-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays.
    Garino C; Tomita T; Pietrancosta N; Laras Y; Rosas R; Herbette G; Maigret B; Quéléver G; Iwatsubo T; Kraus JL
    J Med Chem; 2006 Jul; 49(14):4275-85. PubMed ID: 16821787
    [TBL] [Abstract][Full Text] [Related]  

  • 2. BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline.
    Garino C; Pietrancosta N; Laras Y; Moret V; Rolland A; Quéléver G; Kraus JL
    Bioorg Med Chem Lett; 2006 Apr; 16(7):1995-9. PubMed ID: 16412632
    [TBL] [Abstract][Full Text] [Related]  

  • 3. Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1.
    Yang W; Lu W; Lu Y; Zhong M; Sun J; Thomas AE; Wilkinson JM; Fucini RV; Lam M; Randal M; Shi XP; Jacobs JW; McDowell RS; Gordon EM; Ballinger MD
    J Med Chem; 2006 Feb; 49(3):839-42. PubMed ID: 16451048
    [TBL] [Abstract][Full Text] [Related]  

  • 4. Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase.
    Hom RK; Gailunas AF; Mamo S; Fang LY; Tung JS; Walker DE; Davis D; Thorsett ED; Jewett NE; Moon JB; John V
    J Med Chem; 2004 Jan; 47(1):158-64. PubMed ID: 14695829
    [TBL] [Abstract][Full Text] [Related]  

  • 5. Design, synthesis, and evaluation of Leu*Ala hydroxyethylene-based non-peptide beta-secretase (BACE) inhibitors.
    Xiao K; Li X; Li J; Ma L; Hu B; Yu H; Fu Y; Wang R; Ma Z; Qiu B; Li J; Hu D; Wang X; Shen J
    Bioorg Med Chem; 2006 Jul; 14(13):4535-51. PubMed ID: 16510290
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
    Lindsley SR; Moore KP; Rajapakse HA; Selnick HG; Young MB; Zhu H; Munshi S; Kuo L; McGaughey GB; Colussi D; Crouthamel MC; Lai MT; Pietrak B; Price EA; Sankaranarayanan S; Simon AJ; Seabrook GR; Hazuda DJ; Pudvah NT; Hochman JH; Graham SL; Vacca JP; Nantermet PG
    Bioorg Med Chem Lett; 2007 Jul; 17(14):4057-61. PubMed ID: 17482814
    [TBL] [Abstract][Full Text] [Related]  

  • 7. Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds.
    Piazzi L; Cavalli A; Colizzi F; Belluti F; Bartolini M; Mancini F; Recanatini M; Andrisano V; Rampa A
    Bioorg Med Chem Lett; 2008 Jan; 18(1):423-6. PubMed ID: 17998161
    [TBL] [Abstract][Full Text] [Related]  

  • 8. Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
    Kimura T; Shuto D; Hamada Y; Igawa N; Kasai S; Liu P; Hidaka K; Hamada T; Hayashi Y; Kiso Y
    Bioorg Med Chem Lett; 2005 Jan; 15(1):211-5. PubMed ID: 15582441
    [TBL] [Abstract][Full Text] [Related]  

  • 9. Determination of the active site protonation state of beta-secretase from molecular dynamics simulation and docking experiment: implications for structure-based inhibitor design.
    Park H; Lee S
    J Am Chem Soc; 2003 Dec; 125(52):16416-22. PubMed ID: 14692784
    [TBL] [Abstract][Full Text] [Related]  

  • 10. Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase.
    Zhu Y; Xiao K; Ma L; Xiong B; Fu Y; Yu H; Wang W; Wang X; Hu D; Peng H; Li J; Gong Q; Chai Q; Tang X; Zhang H; Li J; Shen J
    Bioorg Med Chem; 2009 Feb; 17(4):1600-13. PubMed ID: 19162488
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Design and synthesis of highly potent benzodiazepine gamma-secretase inhibitors: preparation of (2S,3R)-3-(3,4-difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]-diazepin-3-yl)butyramide by use of an asymmetric Ireland-Claisen rearrangement.
    Churcher I; Williams S; Kerrad S; Harrison T; Castro JL; Shearman MS; Lewis HD; Clarke EE; Wrigley JD; Beher D; Tang YS; Liu W
    J Med Chem; 2003 Jun; 46(12):2275-8. PubMed ID: 12773031
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Apo and inhibitor complex structures of BACE (beta-secretase).
    Patel S; Vuillard L; Cleasby A; Murray CW; Yon J
    J Mol Biol; 2004 Oct; 343(2):407-16. PubMed ID: 15451669
    [TBL] [Abstract][Full Text] [Related]  

  • 13. 3,4-Fused cyclohexyl sulfones as gamma-secretase inhibitors.
    Shaw D; Best J; Dinnell K; Nadin A; Shearman M; Pattison C; Peachey J; Reilly M; Williams B; Wrigley J; Harrison T
    Bioorg Med Chem Lett; 2006 Jun; 16(11):3073-7. PubMed ID: 16617016
    [TBL] [Abstract][Full Text] [Related]  

  • 14. Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors.
    Hu B; Fan KY; Bridges K; Chopra R; Lovering F; Cole D; Zhou P; Ellingboe J; Jin G; Cowling R; Bard J
    Bioorg Med Chem Lett; 2004 Jul; 14(13):3457-60. PubMed ID: 15177452
    [TBL] [Abstract][Full Text] [Related]  

  • 15. Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.
    Bäck M; Nyhlén J; Kvarnström I; Appelgren S; Borkakoti N; Jansson K; Lindberg J; Nyström S; Hallberg A; Rosenquist S; Samuelsson B
    Bioorg Med Chem; 2008 Nov; 16(21):9471-86. PubMed ID: 18842420
    [TBL] [Abstract][Full Text] [Related]  

  • 16. beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells.
    Hamada Y; Igawa N; Ikari H; Ziora Z; Nguyen JT; Yamani A; Hidaka K; Kimura T; Saito K; Hayashi Y; Ebina M; Ishiura S; Kiso Y
    Bioorg Med Chem Lett; 2006 Aug; 16(16):4354-9. PubMed ID: 16757166
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Conformationally biased P3 amide replacements of beta-secretase inhibitors.
    Stachel SJ; Coburn CA; Steele TG; Crouthamel MC; Pietrak BL; Lai MT; Holloway MK; Munshi SK; Graham SL; Vacca JP
    Bioorg Med Chem Lett; 2006 Feb; 16(3):641-4. PubMed ID: 16263281
    [TBL] [Abstract][Full Text] [Related]  

  • 18. Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.
    Malamas MS; Erdei J; Gunawan I; Turner J; Hu Y; Wagner E; Fan K; Chopra R; Olland A; Bard J; Jacobsen S; Magolda RL; Pangalos M; Robichaud AJ
    J Med Chem; 2010 Feb; 53(3):1146-58. PubMed ID: 19968289
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Biochemical and cell-based assays for characterization of BACE-1 inhibitors.
    Pietrak BL; Crouthamel MC; Tugusheva K; Lineberger JE; Xu M; DiMuzio JM; Steele T; Espeseth AS; Stachel SJ; Coburn CA; Graham SL; Vacca JP; Shi XP; Simon AJ; Hazuda DJ; Lai MT
    Anal Biochem; 2005 Jul; 342(1):144-51. PubMed ID: 15958191
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
    Cumming J; Babu S; Huang Y; Carrol C; Chen X; Favreau L; Greenlee W; Guo T; Kennedy M; Kuvelkar R; Le T; Li G; McHugh N; Orth P; Ozgur L; Parker E; Saionz K; Stamford A; Strickland C; Tadesse D; Voigt J; Zhang L; Zhang Q
    Bioorg Med Chem Lett; 2010 May; 20(9):2837-42. PubMed ID: 20347593
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 11.