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Journal Abstract Search

326 related items for PubMed ID: 19762236

  • 1. The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.
    Malagu K, Duggan H, Menear K, Hummersone M, Gomez S, Bailey C, Edwards P, Drzewiecki J, Leroux F, Quesada MJ, Hermann G, Maine S, Molyneaux CA, Le Gall A, Pullen J, Hickson I, Smith L, Maguire S, Martin N, Smith G, Pass M.
    Bioorg Med Chem Lett; 2009 Oct 15; 19(20):5950-3. PubMed ID: 19762236
    [Abstract] [Full Text] [Related]

  • 2. Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.
    Menear KA, Gomez S, Malagu K, Bailey C, Blackburn K, Cockcroft XL, Ewen S, Fundo A, Le Gall A, Hermann G, Sebastian L, Sunose M, Presnot T, Torode E, Hickson I, Martin NM, Smith GC, Pike KG.
    Bioorg Med Chem Lett; 2009 Oct 15; 19(20):5898-901. PubMed ID: 19733066
    [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. A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.
    Lee W, Ortwine DF, Bergeron P, Lau K, Lin L, Malek S, Nonomiya J, Pei Z, Robarge KD, Schmidt S, Sideris S, Lyssikatos JP.
    Bioorg Med Chem Lett; 2013 Sep 15; 23(18):5097-104. PubMed ID: 23932790
    [Abstract] [Full Text] [Related]

  • 5. Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor.
    Finlay MR, Buttar D, Critchlow SE, Dishington AP, Fillery SM, Fisher E, Glossop SC, Graham MA, Johnson T, Lamont GM, Mutton S, Perkins P, Pike KG, Slater AM.
    Bioorg Med Chem Lett; 2012 Jun 15; 22(12):4163-8. PubMed ID: 22607682
    [Abstract] [Full Text] [Related]

  • 6. Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.
    Pecchi S, Renhowe PA, Taylor C, Kaufman S, Merritt H, Wiesmann M, Shoemaker KR, Knapp MS, Ornelas E, Hendrickson TF, Fantl W, Voliva CF.
    Bioorg Med Chem Lett; 2010 Dec 01; 20(23):6895-8. PubMed ID: 21035331
    [Abstract] [Full Text] [Related]

  • 7. 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]

  • 8. Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2-ones as potent and selective mTOR kinase inhibitors.
    Mortensen DS, Perrin-Ninkovic SM, Harris R, Lee BG, Shevlin G, Hickman M, Khambatta G, Bisonette RR, Fultz KE, Sankar S.
    Bioorg Med Chem Lett; 2011 Nov 15; 21(22):6793-9. PubMed ID: 21978683
    [Abstract] [Full Text] [Related]

  • 9. Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
    Shallal HM, Russu WA.
    Eur J Med Chem; 2011 Jun 15; 46(6):2043-57. PubMed ID: 21429632
    [Abstract] [Full Text] [Related]

  • 10. Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents.
    Peng W, Tu ZC, Long ZJ, Liu Q, Lu G.
    Eur J Med Chem; 2016 Jan 27; 108():644-654. PubMed ID: 26731167
    [Abstract] [Full Text] [Related]

  • 11.
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  • 12. Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines.
    Lee J, Kim H, Yu H, Chung JY, Oh CH, Yoo KH, Sim T, Hah JM.
    Bioorg Med Chem Lett; 2010 Mar 01; 20(5):1573-7. PubMed ID: 20149658
    [Abstract] [Full Text] [Related]

  • 13.
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  • 14. 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]

  • 15. 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]

  • 16. Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.
    Zask A, Kaplan J, Verheijen JC, Richard DJ, Curran K, Brooijmans N, Bennett EM, Toral-Barza L, Hollander I, Ayral-Kaloustian S, Yu K.
    J Med Chem; 2009 Dec 24; 52(24):7942-5. PubMed ID: 19916508
    [Abstract] [Full Text] [Related]

  • 17. Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.
    Koehler MF, Bergeron P, Blackwood E, Bowman KK, Chen YH, Deshmukh G, Ding X, Epler J, Lau K, Lee L, Liu L, Ly C, Malek S, Nonomiya J, Oeh J, Ortwine DF, Sampath D, Sideris S, Trinh L, Truong T, Wu J, Pei Z, Lyssikatos JP.
    J Med Chem; 2012 Dec 27; 55(24):10958-71. PubMed ID: 23199076
    [Abstract] [Full Text] [Related]

  • 18. Synthesis and evaluation of pyrido-thieno-pyrimidines as potent and selective Cdc7 kinase inhibitors.
    Zhao C, Tovar C, Yin X, Xu Q, Todorov IT, Vassilev LT, Chen L.
    Bioorg Med Chem Lett; 2009 Jan 15; 19(2):319-23. PubMed ID: 19071019
    [Abstract] [Full Text] [Related]

  • 19. Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
    Medina JR, Becker CJ, Blackledge CW, Duquenne C, Feng Y, Grant SW, Heerding D, Li WH, Miller WH, Romeril SP, Scherzer D, Shu A, Bobko MA, Chadderton AR, Dumble M, Gardiner CM, Gilbert S, Liu Q, Rabindran SK, Sudakin V, Xiang H, Brady PG, Campobasso N, Ward P, Axten JM.
    J Med Chem; 2011 Mar 24; 54(6):1871-95. PubMed ID: 21341675
    [Abstract] [Full Text] [Related]

  • 20. Inhibition of tumor cell growth, proliferation and migration by X-387, a novel active-site inhibitor of mTOR.
    Chen SM, Liu JL, Wang X, Liang C, Ding J, Meng LH.
    Biochem Pharmacol; 2012 May 01; 83(9):1183-94. PubMed ID: 22305748
    [Abstract] [Full Text] [Related]

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