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Journal Abstract Search

206 related items for PubMed ID: 20050669

  • 1. 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]

  • 2. 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]

  • 3. Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.
    Dehnhardt CM, Venkatesan AM, Delos Santos E, Chen Z, Santos O, Ayral-Kaloustian S, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Chaudhary I, Yu K, Gibbons J, Abraham R, Mansour TS.
    J Med Chem; 2010 Jan 28; 53(2):798-810. PubMed ID: 19968288
    [Abstract] [Full Text] [Related]

  • 4. 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]

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  • 6. Hybrid inhibitors of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR): design, synthesis, and superior antitumor activity of novel wortmannin-rapamycin conjugates.
    Ayral-Kaloustian S, Gu J, Lucas J, Cinque M, Gaydos C, Zask A, Chaudhary I, Wang J, Di L, Young M, Ruppen M, Mansour TS, Gibbons JJ, Yu K.
    J Med Chem; 2010 Jan 14; 53(1):452-9. PubMed ID: 19928864
    [Abstract] [Full Text] [Related]

  • 7. Novel benzofuran-3-one indole inhibitors of PI3 kinase-alpha and the mammalian target of rapamycin: hit to lead studies.
    Bursavich MG, Brooijmans N, Feldberg L, Hollander I, Kim S, Lombardi S, Park K, Mallon R, Gilbert AM.
    Bioorg Med Chem Lett; 2010 Apr 15; 20(8):2586-90. PubMed ID: 20303263
    [Abstract] [Full Text] [Related]

  • 8. 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]

  • 9. Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.
    Richard DJ, Verheijen JC, Curran K, Kaplan J, Toral-Barza L, Hollander I, Lucas J, Yu K, Zask A.
    Bioorg Med Chem Lett; 2009 Dec 15; 19(24):6830-5. PubMed ID: 19896845
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  • 11. 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]

  • 12. NVP-BEZ235, a dual PI3K/mTOR inhibitor, prevents PI3K signaling and inhibits the growth of cancer cells with activating PI3K mutations.
    Serra V, Markman B, Scaltriti M, Eichhorn PJ, Valero V, Guzman M, Botero ML, Llonch E, Atzori F, Di Cosimo S, Maira M, Garcia-Echeverria C, Parra JL, Arribas J, Baselga J.
    Cancer Res; 2008 Oct 01; 68(19):8022-30. PubMed ID: 18829560
    [Abstract] [Full Text] [Related]

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  • 14. 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]

  • 15. Antimyeloma activity of the orally bioavailable dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235.
    McMillin DW, Ooi M, Delmore J, Negri J, Hayden P, Mitsiades N, Jakubikova J, Maira SM, Garcia-Echeverria C, Schlossman R, Munshi NC, Richardson PG, Anderson KC, Mitsiades CS.
    Cancer Res; 2009 Jul 15; 69(14):5835-42. PubMed ID: 19584292
    [Abstract] [Full Text] [Related]

  • 16. 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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  • 18. 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]

  • 19. 5-ureidobenzofuranone indoles as potent and efficacious inhibitors of PI3 kinase-alpha and mTOR for the treatment of breast cancer.
    Zhang N, Ayral-Kaloustian S, Anderson JT, Nguyen T, Das S, Venkatesan AM, Brooijmans N, Lucas J, Yu K, Hollander I, Mallon R.
    Bioorg Med Chem Lett; 2010 Jun 15; 20(12):3526-9. PubMed ID: 20483602
    [Abstract] [Full Text] [Related]

  • 20. Design, synthesis, and biological evaluation of pyrazolopyrimidine-sulfonamides as potent multiple-mitotic kinase (MMK) inhibitors (part I).
    Zhang L, Fan J, Chong JH, Cesena A, Tam BY, Gilson C, Boykin C, Wang D, Aivazian D, Marcotte D, Xiao G, Le Brazidec JY, Piao J, Lundgren K, Hong K, Vu K, Nguyen K, Gan LS, Silvian L, Ling L, Teng M, Reff M, Takeda N, Timple N, Wang Q, Morena R, Khan S, Zhao S, Li T, Lee WC, Taveras AG, Chao J.
    Bioorg Med Chem Lett; 2011 Sep 15; 21(18):5633-7. PubMed ID: 21798738
    [Abstract] [Full Text] [Related]

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