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Items: 1 to 20 of 224

1.

4-methylpteridinones as orally active and selective PI3K/mTOR dual inhibitors.

Liu KK, Bagrodia S, Bailey S, Cheng H, Chen H, Gao L, Greasley S, Hoffman JE, Hu Q, Johnson TO, Knighton D, Liu Z, Marx MA, Nambu MD, Ninkovic S, Pascual B, Rafidi K, Rodgers CM, Smith GL, Sun S, Wang H, Yang A, Yuan J, Zou A.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6096-9. doi: 10.1016/j.bmcl.2010.08.045. Epub 2010 Aug 14.

PMID:
20817449
2.

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. doi: 10.1016/j.bmcl.2011.09.035. Epub 2011 Sep 16.

PMID:
21978683
3.

Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.

Wurz RP, Liu L, Yang K, Nishimura N, Bo Y, Pettus LH, Caenepeel S, Freeman DJ, McCarter JD, Mullady EL, Miguel TS, Wang L, Zhang N, Andrews KL, Whittington DA, Jiang J, Subramanian R, Hughes PE, Norman MH.

Bioorg Med Chem Lett. 2012 Sep 1;22(17):5714-20. doi: 10.1016/j.bmcl.2012.06.078. Epub 2012 Jul 3.

PMID:
22832322
4.

PI3K/Akt/mTOR pathway inhibitors in cancer: a perspective on clinical progress.

Wu P, Hu YZ.

Curr Med Chem. 2010;17(35):4326-41. Review.

PMID:
20939811
5.

Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.

Liu KK, Huang X, Bagrodia S, Chen JH, Greasley S, Cheng H, Sun S, Knighton D, Rodgers C, Rafidi K, Zou A, Xiao J, Yan S.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1270-4. doi: 10.1016/j.bmcl.2010.12.026. Epub 2010 Dec 10.

PMID:
21269826
6.

Use of core modification in the discovery of CC214-2, an orally available, selective inhibitor of mTOR kinase.

Mortensen DS, Sapienza J, Lee BG, Perrin-Ninkovic SM, Harris R, Shevlin G, Parnes JS, Whitefield B, Hickman M, Khambatta G, Bisonette RR, Peng S, Gamez JC, Leisten J, Narla RK, Fultz KE, Sankar S.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1588-91. doi: 10.1016/j.bmcl.2013.01.110. Epub 2013 Jan 30.

PMID:
23414803
7.

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity.

Maira SM, Stauffer F, Brueggen J, Furet P, Schnell C, Fritsch C, Brachmann S, Chène P, De Pover A, Schoemaker K, Fabbro D, Gabriel D, Simonen M, Murphy L, Finan P, Sellers W, García-Echeverría C.

Mol Cancer Ther. 2008 Jul;7(7):1851-63. doi: 10.1158/1535-7163.MCT-08-0017. Epub 2008 Jul 7.

8.

PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity.

Yuan J, Mehta PP, Yin MJ, Sun S, Zou A, Chen J, Rafidi K, Feng Z, Nickel J, Engebretsen J, Hallin J, Blasina A, Zhang E, Nguyen L, Sun M, Vogt PK, McHarg A, Cheng H, Christensen JG, Kan JL, Bagrodia S.

Mol Cancer Ther. 2011 Nov;10(11):2189-99. doi: 10.1158/1535-7163.MCT-11-0185. Epub 2011 Jul 12.

9.

Present and future of PI3K pathway inhibition in cancer: perspectives and limitations.

Ciraolo E, Morello F, Hirsch E.

Curr Med Chem. 2011;18(18):2674-85. Review.

PMID:
21649577
10.

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.

Dehnhardt CM, Venkatesan AM, Chen Z, Delos-Santos E, Ayral-Kaloustian S, Brooijmans N, Yu K, Hollander I, Feldberg L, Lucas J, Mallon R.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4773-8. doi: 10.1016/j.bmcl.2011.06.063. Epub 2011 Jun 21.

PMID:
21763134
11.

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

Cohen F, Bergeron P, Blackwood E, Bowman KK, Chen H, Dipasquale AG, Epler JA, Koehler MF, Lau K, Lewis C, Liu L, Ly CQ, Malek S, Nonomiya J, Ortwine DF, Pei Z, Robarge KD, Sideris S, Trinh L, Truong T, Wu J, Zhao X, Lyssikatos JP.

J Med Chem. 2011 May 12;54(9):3426-35. doi: 10.1021/jm200215y. Epub 2011 Apr 15.

PMID:
21495671
12.

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. doi: 10.1021/jm1014605. Epub 2011 Feb 18.

PMID:
21332118
13.

A selectivity study on mTOR/PI3Kα inhibitors by homology modeling and 3D-QSAR.

Ran T, Lu T, Yuan H, Liu H, Wang J, Zhang W, Leng Y, Lin G, Zhuang S, Chen Y.

J Mol Model. 2012 Jan;18(1):171-86. doi: 10.1007/s00894-011-1034-3. Epub 2011 Apr 27.

PMID:
21523553
14.

PI3K/AKT/mTOR inhibitors in ovarian cancer.

Mazzoletti M, Broggini M.

Curr Med Chem. 2010;17(36):4433-47. Review.

PMID:
21062259
15.

The dual PI3K/mTOR inhibitor BEZ235 is effective in lung cancer cell lines.

Herrera VA, Zeindl-Eberhart E, Jung A, Huber RM, Bergner A.

Anticancer Res. 2011 Mar;31(3):849-54.

PMID:
21498705
16.

PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.

Venkatesan AM, Chen Z, dos Santos O, Dehnhardt C, Santos ED, Ayral-Kaloustian S, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Chaudhary I, Mansour TS.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5869-73. doi: 10.1016/j.bmcl.2010.07.104. Epub 2010 Jul 30.

PMID:
20797855
17.

Allosteric and ATP-competitive kinase inhibitors of mTOR for cancer treatment.

García-Echeverría C.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4308-12. doi: 10.1016/j.bmcl.2010.05.099. Epub 2010 Jun 1. Review.

PMID:
20561789
18.

Structure-based optimization of morpholino-triazines as PI3K and mTOR inhibitors.

Poulsen A, Williams M, Nagaraj HM, William AD, Wang H, Soh CK, Xiong ZC, Dymock B.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1009-13. doi: 10.1016/j.bmcl.2011.12.001. Epub 2011 Dec 8.

PMID:
22197143
19.

ATP-competitive inhibitors of mTOR: an update.

Schenone S, Brullo C, Musumeci F, Radi M, Botta M.

Curr Med Chem. 2011;18(20):2995-3014. Review.

PMID:
21651476
20.

2-Arylthiazolidine-4-carboxylic acid amides (ATCAA) target dual pathways in cancer cells: 5'-AMP-activated protein kinase (AMPK)/mTOR and PI3K/Akt/mTOR pathways.

Li CM, Narayanan R, Lu Y, Hurh E, Coss CC, Barrett CM, Miller DD, Dalton JT.

Int J Oncol. 2010 Oct;37(4):1023-30.

PMID:
20811725

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