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188 related items for PubMed ID: 19963384

  • 1. Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
    Kaplan J, Verheijen JC, Brooijmans N, Toral-Barza L, Hollander I, Yu K, Zask A.
    Bioorg Med Chem Lett; 2010 Jan 15; 20(2):640-3. PubMed ID: 19963384
    [Abstract] [Full Text] [Related]

  • 2. Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 1-substituent.
    Curran KJ, Verheijen JC, Kaplan J, Richard DJ, Toral-Barza L, Hollander I, Lucas J, Ayral-Kaloustian S, Yu K, Zask A.
    Bioorg Med Chem Lett; 2010 Feb 15; 20(4):1440-4. PubMed ID: 20089401
    [Abstract] [Full Text] [Related]

  • 3. 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]

  • 4. Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K.
    Verheijen JC, Yu K, Toral-Barza L, Hollander I, Zask A.
    Bioorg Med Chem Lett; 2010 Jan 01; 20(1):375-9. PubMed ID: 19897362
    [Abstract] [Full Text] [Related]

  • 5. ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.
    Zask A, Verheijen JC, Curran K, Kaplan J, Richard DJ, Nowak P, Malwitz DJ, Brooijmans N, Bard J, Svenson K, Lucas J, Toral-Barza L, Zhang WG, Hollander I, Gibbons JJ, Abraham RT, Ayral-Kaloustian S, Mansour TS, Yu K.
    J Med Chem; 2009 Aug 27; 52(16):5013-6. PubMed ID: 19645448
    [Abstract] [Full Text] [Related]

  • 6. Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors.
    Zask A, Verheijen JC, Richard DJ, Kaplan J, Curran K, Toral-Barza L, Lucas J, Hollander I, Yu K.
    Bioorg Med Chem Lett; 2010 Apr 15; 20(8):2644-7. PubMed ID: 20227881
    [Abstract] [Full Text] [Related]

  • 7. Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies.
    Gilbert AM, Nowak P, Brooijmans N, Bursavich MG, Dehnhardt C, Santos ED, Feldberg LR, Hollander I, Kim S, Lombardi S, Park K, Venkatesan AM, Mallon R.
    Bioorg Med Chem Lett; 2010 Jan 15; 20(2):636-9. PubMed ID: 19969455
    [Abstract] [Full Text] [Related]

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  • 9. Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.
    Venkatesan AM, Dehnhardt CM, Chen Z, Santos ED, Dos Santos O, Bursavich M, Gilbert AM, Ellingboe JW, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham R, Mansour TS.
    Bioorg Med Chem Lett; 2010 Jan 15; 20(2):653-6. PubMed ID: 19954970
    [Abstract] [Full Text] [Related]

  • 10. Recent advances in the development of selective, ATP-competitive inhibitors of mTOR.
    Richard DJ, Verheijen JC, Zask A.
    Curr Opin Drug Discov Devel; 2010 Jul 15; 13(4):428-40. PubMed ID: 20597028
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  • 12. Discovery and optimization of 2-(4-substituted-pyrrolo[2,3-b]pyridin-3-yl)methylene-4-hydroxybenzofuran-3(2H)-ones as potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
    Tsou HR, MacEwan G, Birnberg G, Grosu G, Bursavich MG, Bard J, Brooijmans N, Toral-Barza L, Hollander I, Mansour TS, Ayral-Kaloustian S, Yu K.
    Bioorg Med Chem Lett; 2010 Apr 01; 20(7):2321-5. PubMed ID: 20188552
    [Abstract] [Full Text] [Related]

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  • 14. 4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
    Tsou HR, MacEwan G, Birnberg G, Zhang N, Brooijmans N, Toral-Barza L, Hollander I, Ayral-Kaloustian S, Yu K.
    Bioorg Med Chem Lett; 2010 Apr 01; 20(7):2259-63. PubMed ID: 20188551
    [Abstract] [Full Text] [Related]

  • 15. Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha.
    Richard DJ, Verheijen JC, Yu K, Zask A.
    Bioorg Med Chem Lett; 2010 Apr 15; 20(8):2654-7. PubMed ID: 20223664
    [Abstract] [Full Text] [Related]

  • 16. Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.
    Nowak P, Cole DC, Brooijmans N, Bursavich MG, Curran KJ, Ellingboe JW, Gibbons JJ, Hollander I, Hu Y, Kaplan J, Malwitz DJ, Toral-Barza L, Verheijen JC, Zask A, Zhang WG, Yu K.
    J Med Chem; 2009 Nov 26; 52(22):7081-9. PubMed ID: 19848404
    [Abstract] [Full Text] [Related]

  • 17. Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.
    Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, Folkes A, Gunzner J, Lesnick JD, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Sutherlin DP, Tsui V, Wan NC, Wang S, Wong S, Zhu BY.
    Bioorg Med Chem Lett; 2010 Apr 15; 20(8):2408-11. PubMed ID: 20346656
    [Abstract] [Full Text] [Related]

  • 18. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.
    Sutherlin DP, Sampath D, Berry M, Castanedo G, Chang Z, Chuckowree I, Dotson J, Folkes A, Friedman L, Goldsmith R, Heffron T, Lee L, Lesnick J, Lewis C, Mathieu S, Nonomiya J, Olivero A, Pang J, Prior WW, Salphati L, Sideris S, Tian Q, Tsui V, Wan NC, Wang S, Wiesmann C, Wong S, Zhu BY.
    J Med Chem; 2010 Feb 11; 53(3):1086-97. PubMed ID: 20050669
    [Abstract] [Full Text] [Related]

  • 19. Assessment of the putative binding conformation of a pyrazolopyridine class of inhibitors of MAPKAPK2 using computational studies.
    Miglani R, Cliffe IA, Voleti SR.
    Eur J Med Chem; 2010 Jan 11; 45(1):98-105. PubMed ID: 19850376
    [Abstract] [Full Text] [Related]

  • 20. Discovery and evaluation of pyrazolo[1,5-a]pyrimidines as neuropeptide Y1 receptor antagonists.
    Griffith DA, Hargrove DM, Maurer TS, Blum CA, De Lombaert S, Inthavongsay JK, Klade LE, Mack CM, Rose CR, Sanders MJ, Carpino PA.
    Bioorg Med Chem Lett; 2011 May 01; 21(9):2641-5. PubMed ID: 21295475
    [Abstract] [Full Text] [Related]

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