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395 related items for PubMed ID: 19854649

  • 1. Discovery of highly potent and selective type I B-Raf kinase inhibitors.
    Wang X, Berger DM, Salaski EJ, Torres N, Hu Y, Levin JI, Powell D, Wojciechowicz D, Collins K, Frommer E.
    Bioorg Med Chem Lett; 2009 Dec 01; 19(23):6571-4. PubMed ID: 19854649
    [Abstract] [Full Text] [Related]

  • 2. Non-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors.
    Berger DM, Torres N, Dutia M, Powell D, Ciszewski G, Gopalsamy A, Levin JI, Kim KH, Xu W, Wilhelm J, Hu Y, Collins K, Feldberg L, Kim S, Frommer E, Wojciechowicz D, Mallon R.
    Bioorg Med Chem Lett; 2009 Dec 01; 19(23):6519-23. PubMed ID: 19864136
    [Abstract] [Full Text] [Related]

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  • 4. 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
    Ledeboer MW, Pierce AC, Duffy JP, Gao H, Messersmith D, Salituro FG, Nanthakumar S, Come J, Zuccola HJ, Swenson L, Shlyakter D, Mahajan S, Hoock T, Fan B, Tsai WJ, Kolaczkowski E, Carrier S, Hogan JK, Zessis R, Pazhanisamy S, Bennani YL.
    Bioorg Med Chem Lett; 2009 Dec 01; 19(23):6529-33. PubMed ID: 19857967
    [Abstract] [Full Text] [Related]

  • 5. Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties.
    Ren L, Laird ER, Buckmelter AJ, Dinkel V, Gloor SL, Grina J, Newhouse B, Rasor K, Hastings G, Gradl SN, Rudolph J.
    Bioorg Med Chem Lett; 2012 Jan 15; 22(2):1165-8. PubMed ID: 22196124
    [Abstract] [Full Text] [Related]

  • 6. Discovery and optimization of N-acyl and N-aroylpyrazolines as B-Raf kinase inhibitors.
    Blackburn C, Duffey MO, Gould AE, Kulkarni B, Liu JX, Menon S, Nagayoshi M, Vos TJ, Williams J.
    Bioorg Med Chem Lett; 2010 Aug 15; 20(16):4795-9. PubMed ID: 20630752
    [Abstract] [Full Text] [Related]

  • 7. Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.
    Das J, Moquin RV, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.
    Bioorg Med Chem Lett; 2008 Apr 15; 18(8):2652-7. PubMed ID: 18359226
    [Abstract] [Full Text] [Related]

  • 8. Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.
    Dwyer MP, Paruch K, Alvarez C, Doll RJ, Keertikar K, Duca J, Fischmann TO, Hruza A, Madison V, Lees E, Parry D, Seghezzi W, Sgambellone N, Shanahan F, Wiswell D, Guzi TJ.
    Bioorg Med Chem Lett; 2007 Nov 15; 17(22):6216-9. PubMed ID: 17904366
    [Abstract] [Full Text] [Related]

  • 9. Discovery and optimization of pyrazoline compounds as B-Raf inhibitors.
    Duffey MO, Adams R, Blackburn C, Chau RW, Chen S, Galvin KM, Garcia K, Gould AE, Greenspan PD, Harrison S, Huang SC, Kim MS, Kulkarni B, Langston S, Liu JX, Ma LT, Menon S, Nagayoshi M, Rowland RS, Vos TJ, Xu T, Yang JJ, Yu S, Zhang Q.
    Bioorg Med Chem Lett; 2010 Aug 15; 20(16):4800-4. PubMed ID: 20634068
    [Abstract] [Full Text] [Related]

  • 10. Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.
    Verheijen JC, Richard DJ, Curran K, Kaplan J, Lefever M, Nowak P, Malwitz DJ, Brooijmans N, Toral-Barza L, Zhang WG, Lucas J, Hollander I, Ayral-Kaloustian S, Mansour TS, Yu K, Zask A.
    J Med Chem; 2009 Dec 24; 52(24):8010-24. PubMed ID: 19894727
    [Abstract] [Full Text] [Related]

  • 11. B-Raf kinase inhibitors: hit enrichment through scaffold hopping.
    Gopalsamy A, Shi M, Hu Y, Lee F, Feldberg L, Frommer E, Kim S, Collins K, Wojciechowicz D, Mallon R.
    Bioorg Med Chem Lett; 2010 Apr 15; 20(8):2431-4. PubMed ID: 20307980
    [Abstract] [Full Text] [Related]

  • 12. Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline.
    Smith AL, DeMorin FF, Paras NA, Huang Q, Petkus JK, Doherty EM, Nixey T, Kim JL, Whittington DA, Epstein LF, Lee MR, Rose MJ, Babij C, Fernando M, Hess K, Le Q, Beltran P, Carnahan J.
    J Med Chem; 2009 Oct 22; 52(20):6189-92. PubMed ID: 19764794
    [Abstract] [Full Text] [Related]

  • 13. Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors.
    Gopalsamy A, Ciszewski G, Shi M, Berger D, Hu Y, Lee F, Feldberg L, Frommer E, Kim S, Collins K, Wojciechowicz D, Mallon R.
    Bioorg Med Chem Lett; 2009 Dec 15; 19(24):6890-2. PubMed ID: 19884006
    [Abstract] [Full Text] [Related]

  • 14. Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors.
    Wenglowsky S, Moreno D, Laird ER, Gloor SL, Ren L, Risom T, Rudolph J, Sturgis HL, Voegtli WC.
    Bioorg Med Chem Lett; 2012 Oct 01; 22(19):6237-41. PubMed ID: 22954737
    [Abstract] [Full Text] [Related]

  • 15. 7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.
    Frey RR, Curtin ML, Albert DH, Glaser KB, Pease LJ, Soni NB, Bouska JJ, Reuter D, Stewart KD, Marcotte P, Bukofzer G, Li J, Davidsen SK, Michaelides MR.
    J Med Chem; 2008 Jul 10; 51(13):3777-87. PubMed ID: 18557606
    [Abstract] [Full Text] [Related]

  • 16. Pyrazolopyridine inhibitors of B-RafV600E. Part 2: structure-activity relationships.
    Wenglowsky S, Ahrendt KA, Buckmelter AJ, Feng B, Gloor SL, Gradl S, Grina J, Hansen JD, Laird ER, Lunghofer P, Mathieu S, Moreno D, Newhouse B, Ren L, Risom T, Rudolph J, Seo J, Sturgis HL, Voegtli WC, Wen Z.
    Bioorg Med Chem Lett; 2011 Sep 15; 21(18):5533-7. PubMed ID: 21802293
    [Abstract] [Full Text] [Related]

  • 17. Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.
    Dwyer MP, Keertikar K, Paruch K, Alvarez C, Labroli M, Poker C, Fischmann TO, Mayer-Ezell R, Bond R, Wang Y, Azevedo R, Guzi TJ.
    Bioorg Med Chem Lett; 2013 Nov 15; 23(22):6178-82. PubMed ID: 24091081
    [Abstract] [Full Text] [Related]

  • 18. Discovery and in vitro evaluation of potent kinase inhibitors: Pyrido[1',2':1,5]pyrazolo[3,4-d]pyrimidines.
    Alberti MJ, Auten EP, Lackey KE, McDonald OB, Wood ER, Preugschat F, Cutler GJ, Kane-Carson L, Liu W, Jung DK.
    Bioorg Med Chem Lett; 2005 Aug 15; 15(16):3778-81. PubMed ID: 15993060
    [Abstract] [Full Text] [Related]

  • 19. Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.
    Zhang G, Ren P, Gray NS, Sim T, Wang X, Liu Y, Che J, Dong W, Tian SS, Sandberg ML, Spalding TA, Romeo R, Iskandar M, Wang Z, Seidel HM, Karanewsky DS, He Y.
    Bioorg Med Chem Lett; 2009 Dec 01; 19(23):6691-5. PubMed ID: 19854052
    [Abstract] [Full Text] [Related]

  • 20. Knowledge-based design of 7-azaindoles as selective B-Raf inhibitors.
    Tang J, Hamajima T, Nakano M, Sato H, Dickerson SH, Lackey KE.
    Bioorg Med Chem Lett; 2008 Aug 15; 18(16):4610-4. PubMed ID: 18662874
    [Abstract] [Full Text] [Related]

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