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Response and determinants of cancer cell susceptibility to PI3K inhibitors: combined targeting of PI3K and Mek1 as an effective anticancer strategy.
Yu K, Toral-Barza L, Shi C, Zhang WG, Zask A. Yu K, et al. Cancer Biol Ther. 2008 Feb;7(2):307-15. doi: 10.4161/cbt.7.2.5334. Epub 2007 Nov 21. Cancer Biol Ther. 2008. PMID: 18059185
Requirement of the mTOR kinase for the regulation of Maf1 phosphorylation and control of RNA polymerase III-dependent transcription in cancer cells.
Shor B, Wu J, Shakey Q, Toral-Barza L, Shi C, Follettie M, Yu K. Shor B, et al. Among authors: toral barza l. J Biol Chem. 2010 May 14;285(20):15380-92. doi: 10.1074/jbc.M109.071639. Epub 2010 Mar 16. J Biol Chem. 2010. PMID: 20233713 Free PMC article.
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. Zask A, et al. Among authors: toral barza l. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2644-7. doi: 10.1016/j.bmcl.2010.02.045. Epub 2010 Feb 13. Bioorg Med Chem Lett. 2010. PMID: 20227881
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. Tsou HR, et al. Among authors: toral barza l. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2321-5. doi: 10.1016/j.bmcl.2010.01.135. Epub 2010 Feb 2. Bioorg Med Chem Lett. 2010. PMID: 20188552
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. Tsou HR, et al. Among authors: toral barza l. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2259-63. doi: 10.1016/j.bmcl.2010.02.012. Epub 2010 Feb 6. Bioorg Med Chem Lett. 2010. PMID: 20188551
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. Curran KJ, et al. Among authors: toral barza l. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1440-4. doi: 10.1016/j.bmcl.2009.12.086. Epub 2010 Jan 4. Bioorg Med Chem Lett. 2010. PMID: 20089401
Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2.
Yu K, Shi C, Toral-Barza L, Lucas J, Shor B, Kim JE, Zhang WG, Mahoney R, Gaydos C, Tardio L, Kim SK, Conant R, Curran K, Kaplan J, Verheijen J, Ayral-Kaloustian S, Mansour TS, Abraham RT, Zask A, Gibbons JJ. Yu K, et al. Among authors: toral barza l. Cancer Res. 2010 Jan 15;70(2):621-31. doi: 10.1158/0008-5472.CAN-09-2340. Epub 2010 Jan 12. Cancer Res. 2010. PMID: 20068177 Free article.
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. Kaplan J, et al. Bioorg Med Chem Lett. 2010 Jan 15;20(2):640-3. doi: 10.1016/j.bmcl.2009.11.050. Epub 2009 Dec 4. Bioorg Med Chem Lett. 2010. PMID: 19963384
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. Zask A, et al. J Med Chem. 2009 Dec 24;52(24):7942-5. doi: 10.1021/jm901415x. J Med Chem. 2009. PMID: 19916508
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. Verheijen JC, et al. Bioorg Med Chem Lett. 2010 Jan 1;20(1):375-9. doi: 10.1016/j.bmcl.2009.10.075. Epub 2009 Oct 22. Bioorg Med Chem Lett. 2010. PMID: 19897362
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