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Journal Abstract Search


123 related items for PubMed ID: 19968288

  • 1. 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]

  • 2. WJD008, a dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin inhibitor, prevents PI3K signaling and inhibits the proliferation of transformed cells with oncogenic PI3K mutant.
    Li T, Wang J, Wang X, Yang N, Chen SM, Tong LJ, Yang CH, Meng LH, Ding J.
    J Pharmacol Exp Ther; 2010 Sep 01; 334(3):830-8. PubMed ID: 20522531
    [Abstract] [Full Text] [Related]

  • 3. 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]

  • 4. Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.
    Chen Z, Venkatesan AM, Dehnhardt CM, Ayral-Kaloustian S, Brooijmans N, Mallon R, Feldberg L, Hollander I, Lucas J, Yu K, Kong F, Mansour TS.
    J Med Chem; 2010 Apr 22; 53(8):3169-82. PubMed ID: 20334367
    [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. 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. 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]

  • 8. 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]

  • 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. 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]

  • 11. 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]

  • 12. 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]

  • 13. The PI3K/Akt and mTOR/P70S6K signaling pathways in human uveal melanoma cells: interaction with B-Raf/ERK.
    Babchia N, Calipel A, Mouriaux F, Faussat AM, Mascarelli F.
    Invest Ophthalmol Vis Sci; 2010 Jan 15; 51(1):421-9. PubMed ID: 19661225
    [Abstract] [Full Text] [Related]

  • 14. 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
    [Abstract] [Full Text] [Related]

  • 15. Mammalian target of rapamycin, a molecular target in squamous cell carcinomas of the head and neck.
    Amornphimoltham P, Patel V, Sodhi A, Nikitakis NG, Sauk JJ, Sausville EA, Molinolo AA, Gutkind JS.
    Cancer Res; 2005 Nov 01; 65(21):9953-61. PubMed ID: 16267020
    [Abstract] [Full Text] [Related]

  • 16. Targeting the PI3K/AKT/mTOR signaling network in acute myelogenous leukemia.
    Martelli AM, Evangelisti C, Chiarini F, Grimaldi C, Manzoli L, McCubrey JA.
    Expert Opin Investig Drugs; 2009 Sep 01; 18(9):1333-49. PubMed ID: 19678801
    [Abstract] [Full Text] [Related]

  • 17. 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]

  • 18. Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.
    D'Angelo ND, Kim TS, Andrews K, Booker SK, Caenepeel S, Chen K, D'Amico D, Freeman D, Jiang J, Liu L, McCarter JD, San Miguel T, Mullady EL, Schrag M, Subramanian R, Tang J, Wahl RC, Wang L, Whittington DA, Wu T, Xi N, Xu Y, Yakowec P, Yang K, Zalameda LP, Zhang N, Hughes P, Norman MH.
    J Med Chem; 2011 Mar 24; 54(6):1789-811. PubMed ID: 21332118
    [Abstract] [Full Text] [Related]

  • 19. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor.
    Mallon R, Hollander I, Feldberg L, Lucas J, Soloveva V, Venkatesan A, Dehnhardt C, Delos Santos E, Chen Z, Dos Santos O, Ayral-Kaloustian S, Gibbons J.
    Mol Cancer Ther; 2010 Apr 24; 9(4):976-84. PubMed ID: 20371716
    [Abstract] [Full Text] [Related]

  • 20. 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]


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