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429 related items for PubMed ID: 19894727

  • 1. 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
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  • 2. 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
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  • 3. 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
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  • 4. 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
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  • 5. 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
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  • 6. 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
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  • 9. 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
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  • 11. 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
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  • 12. 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
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  • 15. 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
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  • 18. Use of a pharmacophore model for the design of EGF-R tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines.
    Traxler P, Bold G, Frei J, Lang M, Lydon N, Mett H, Buchdunger E, Meyer T, Mueller M, Furet P.
    J Med Chem; 1997 Oct 24; 40(22):3601-16. PubMed ID: 9357527
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  • 20. 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
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