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Items: 1 to 20 of 180

1.

Azole-based inhibitors of AKT/PKB for the treatment of cancer.

Zeng Q, Allen JG, Bourbeau MP, Wang X, Yao G, Tadesse S, Rider JT, Yuan CC, Hong FT, Lee MR, Zhang S, Lofgren JA, Freeman DJ, Yang S, Li C, Tominey E, Huang X, Hoffman D, Yamane HK, Fotsch C, Dominguez C, Hungate R, Zhang X.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1559-64. doi: 10.1016/j.bmcl.2010.01.067. Epub 2010 Jan 21.

PMID:
20137943
2.

2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics.

Zeng Q, Bourbeau MP, Wohlhieter GE, Yao G, Monenschein H, Rider JT, Lee MR, Zhang S, Lofgren J, Freeman D, Li C, Tominey E, Huang X, Hoffman D, Yamane H, Tasker AS, Dominguez C, Viswanadhan VN, Hungate R, Zhang X.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1652-6. doi: 10.1016/j.bmcl.2010.01.046. Epub 2010 Jan 20.

PMID:
20137932
3.

Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.

Li Q, Woods KW, Thomas S, Zhu GD, Packard G, Fisher J, Li T, Gong J, Dinges J, Song X, Abrams J, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Des Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):2000-7. Epub 2006 Jan 18.

PMID:
16413780
4.

Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B.

Collins I, Caldwell J, Fonseca T, Donald A, Bavetsias V, Hunter LJ, Garrett MD, Rowlands MG, Aherne GW, Davies TG, Berdini V, Woodhead SJ, Davis D, Seavers LC, Wyatt PG, Workman P, McDonald E.

Bioorg Med Chem. 2006 Feb 15;14(4):1255-73. Epub 2005 Oct 24.

PMID:
16249095
5.

Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.

Xu R, Banka A, Blake JF, Mitchell IS, Wallace EM, Bencsik JR, Kallan NC, Spencer KL, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2335-40. doi: 10.1016/j.bmcl.2011.02.098. Epub 2011 Feb 26.

PMID:
21420856
6.

Discovery of pyrrolopyrimidine inhibitors of Akt.

Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5607-12. doi: 10.1016/j.bmcl.2010.08.053. Epub 2010 Aug 13.

PMID:
20810279
7.

Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.

Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I.

J Med Chem. 2007 May 17;50(10):2289-92. Epub 2007 Apr 24.

PMID:
17451235
8.

Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.

Zhu GD, Gong J, Claiborne A, Woods KW, Gandhi VB, Thomas S, Luo Y, Liu X, Shi Y, Guan R, Magnone SR, Klinghofer V, Johnson EF, Bouska J, Shoemaker A, Oleksijew A, Stoll VS, De Jong R, Oltersdorf T, Li Q, Rosenberg SH, Giranda VL.

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3150-5. Epub 2006 Apr 5.

PMID:
16603355
9.

Tirucallic acids are novel pleckstrin homology domain-dependent Akt inhibitors inducing apoptosis in prostate cancer cells.

Estrada AC, Syrovets T, Pitterle K, Lunov O, Büchele B, Schimana-Pfeifer J, Schmidt T, Morad SA, Simmet T.

Mol Pharmacol. 2010 Mar;77(3):378-87. doi: 10.1124/mol.109.060475. Epub 2009 Dec 16.

10.

Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity.

Rhodes N, Heerding DA, Duckett DR, Eberwein DJ, Knick VB, Lansing TJ, McConnell RT, Gilmer TM, Zhang SY, Robell K, Kahana JA, Geske RS, Kleymenova EV, Choudhry AE, Lai Z, Leber JD, Minthorn EA, Strum SL, Wood ER, Huang PS, Copeland RA, Kumar R.

Cancer Res. 2008 Apr 1;68(7):2366-74. doi: 10.1158/0008-5472.CAN-07-5783.

11.

Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.

Bilodeau MT, Balitza AE, Hoffman JM, Manley PJ, Barnett SF, Defeo-Jones D, Haskell K, Jones RE, Leander K, Robinson RG, Smith AM, Huber HE, Hartman GD.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3178-82. doi: 10.1016/j.bmcl.2008.04.074. Epub 2008 May 1.

PMID:
18479914
12.

Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.

Li Q, Li T, Zhu GD, Gong J, Claibone A, Dalton C, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Bauch JL, Marsh KC, Bouska JJ, Arries S, De Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1679-85. Epub 2006 Jan 5.

PMID:
16403626
13.

A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera.

Davies TG, Verdonk ML, Graham B, Saalau-Bethell S, Hamlett CC, McHardy T, Collins I, Garrett MD, Workman P, Woodhead SJ, Jhoti H, Barford D.

J Mol Biol. 2007 Mar 30;367(3):882-94. Epub 2007 Jan 9.

PMID:
17275837
14.

Design of selective, ATP-competitive inhibitors of Akt.

Freeman-Cook KD, Autry C, Borzillo G, Gordon D, Barbacci-Tobin E, Bernardo V, Briere D, Clark T, Corbett M, Jakubczak J, Kakar S, Knauth E, Lippa B, Luzzio MJ, Mansour M, Martinelli G, Marx M, Nelson K, Pandit J, Rajamohan F, Robinson S, Subramanyam C, Wei L, Wythes M, Morris J.

J Med Chem. 2010 Jun 24;53(12):4615-22. doi: 10.1021/jm1003842. Erratum in: J Med Chem. 2010 Aug 12;53(15):5895.

PMID:
20481595
15.

Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.

Liu JJ, Daniewski I, Ding Q, Higgins B, Ju G, Kolinsky K, Konzelmann F, Lukacs C, Pizzolato G, Rossman P, Swain A, Thakkar K, Wei CC, Miklowski D, Yang H, Yin X, Wovkulich PM.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):5984-7. doi: 10.1016/j.bmcl.2010.08.079. Epub 2010 Aug 21.

PMID:
20832307
16.

Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.

Ashton KS, St Jean DJ Jr, Poon SF, Lee MR, Allen JG, Zhang S, Lofgren JA, Zhang X, Fotsch C, Hungate R.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5191-6. doi: 10.1016/j.bmcl.2011.07.056. Epub 2011 Jul 23.

PMID:
21824779
17.

Identification of inhibitors of protein kinase B using fragment-based lead discovery.

Saxty G, Woodhead SJ, Berdini V, Davies TG, Verdonk ML, Wyatt PG, Boyle RG, Barford D, Downham R, Garrett MD, Carr RA.

J Med Chem. 2007 May 17;50(10):2293-6. Epub 2007 Apr 24.

PMID:
17451234
18.

Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR.

Kendall JD, Giddens AC, Tsang KY, Frédérick R, Marshall ES, Singh R, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle GW, Baguley BC, Flanagan JU, Jamieson SM, Denny WA, Shepherd PR.

Bioorg Med Chem. 2012 Jan 1;20(1):58-68. doi: 10.1016/j.bmc.2011.11.031. Epub 2011 Nov 25.

PMID:
22177407
19.

Synthesis and structure based optimization of novel Akt inhibitors.

Lippa B, Pan G, Corbett M, Li C, Kauffman GS, Pandit J, Robinson S, Wei L, Kozina E, Marr ES, Borzillo G, Knauth E, Barbacci-Tobin EG, Vincent P, Troutman M, Baker D, Rajamohan F, Kakar S, Clark T, Morris J.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3359-63. doi: 10.1016/j.bmcl.2008.04.034. Epub 2008 Apr 15.

PMID:
18456494
20.

Docking of protein kinase B inhibitors: implications in the structure-based optimization of a novel scaffold.

Hernández-Campos A, Velázquez-Martínez I, Castillo R, López-Vallejo F, Jia P, Yu Y, Giulianotti MA, Medina-Franco JL.

Chem Biol Drug Des. 2010 Sep 1;76(3):269-76. doi: 10.1111/j.1747-0285.2010.01002.x. Epub 2010 Jun 22.

PMID:
20572809

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