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Items: 1 to 20 of 157

1.

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
2.

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
3.

Discovery and SAR of spirochromane Akt inhibitors.

Kallan NC, Spencer KL, Blake JF, Xu R, Heizer J, Bencsik JR, Mitchell IS, 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):2410-4. doi: 10.1016/j.bmcl.2011.02.073. Epub 2011 Feb 18.

PMID:
21392984
4.

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
5.

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
6.

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
7.

Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors.

Woods KW, Fischer JP, Claiborne A, Li T, Thomas SA, Zhu GD, Diebold RB, Liu X, Shi Y, Klinghofer V, Han EK, Guan R, Magnone SR, Johnson EF, Bouska JJ, Olson AM, de Jong R, Oltersdorf T, Luo Y, Rosenberg SH, Giranda VL, Li Q.

Bioorg Med Chem. 2006 Oct 15;14(20):6832-46. Epub 2006 Jul 14.

PMID:
16843670
8.

Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt.

Zhu GD, Gong J, Gandhi VB, Woods K, Luo Y, Liu X, Guan R, Klinghofer V, Johnson EF, Stoll VS, Mamo M, Li Q, Rosenberg SH, Giranda VL.

Bioorg Med Chem. 2007 Mar 15;15(6):2441-52. Epub 2007 Jan 17.

PMID:
17258463
9.

Discovery and optimization of p38 inhibitors via computer-assisted drug design.

Goldberg DR, Hao MH, Qian KC, Swinamer AD, Gao DA, Xiong Z, Sarko C, Berry A, Lord J, Magolda RL, Fadra T, Kroe RR, Kukulka A, Madwed JB, Martin L, Pargellis C, Skow D, Song JJ, Tan Z, Torcellini CA, Zimmitti CS, Yee NK, Moss N.

J Med Chem. 2007 Aug 23;50(17):4016-26. Epub 2007 Jul 20.

PMID:
17658737
10.

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
11.

Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.

Bencsik JR, Xiao D, Blake JF, Kallan NC, Mitchell IS, Spencer KL, Xu R, Gloor SL, Martinson M, Risom T, Woessner RD, Dizon F, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ, Prior WW, Murray LJ.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7037-41. doi: 10.1016/j.bmcl.2010.09.112. Epub 2010 Sep 29.

PMID:
20971641
12.

Aminofurazans as potent inhibitors of AKT kinase.

Rouse MB, Seefeld MA, Leber JD, McNulty KC, Sun L, Miller WH, Zhang S, Minthorn EA, Concha NO, Choudhry AE, Schaber MD, Heerding DA.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1508-11. doi: 10.1016/j.bmcl.2009.01.002. Epub 2009 Jan 9.

PMID:
19179070
13.

Discovery of a novel protein kinase B inhibitor by structure-based virtual screening.

Medina-Franco JL, Giulianotti MA, Yu Y, Shen L, Yao L, Singh N.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4634-8. doi: 10.1016/j.bmcl.2009.06.078. Epub 2009 Jun 25.

PMID:
19604696
14.

4-(Benzimidazol-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: potent and selective p70S6 kinase inhibitors.

Bandarage U, Hare B, Parsons J, Pham L, Marhefka C, Bemis G, Tang Q, Moody CS, Rodems S, Shah S, Adams C, Bravo J, Charonnet E, Savic V, Come JH, Green J.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5191-4. doi: 10.1016/j.bmcl.2009.07.022. Epub 2009 Jul 9.

PMID:
19632115
15.

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
16.

Development of sulfonamide AKT PH domain inhibitors.

Ahad AM, Zuohe S, Du-Cuny L, Moses SA, Zhou LL, Zhang S, Powis G, Meuillet EJ, Mash EA.

Bioorg Med Chem. 2011 Mar 15;19(6):2046-54. doi: 10.1016/j.bmc.2011.01.049. Epub 2011 Feb 1.

17.

Discovery of N-(3-((7H-purin-6-yl)thio)-4-hydroxynaphthalen-1-yl)-sulfonamide derivatives as novel protein kinase and angiogenesis inhibitors for the treatment of cancer: Synthesis and biological evaluation. Part III.

Xu F, Xu H, Wang X, Zhang L, Wen Q, Zhang Y, Xu W.

Bioorg Med Chem. 2014 Feb 15;22(4):1487-95. doi: 10.1016/j.bmc.2013.11.052. Epub 2013 Dec 8.

PMID:
24440479
18.

Design and crystal structures of protein kinase B-selective inhibitors in complex with protein kinase A and mutants.

Breitenlechner CB, Friebe WG, Brunet E, Werner G, Graul K, Thomas U, Künkele KP, Schäfer W, Gassel M, Bossemeyer D, Huber R, Engh RA, Masjost B.

J Med Chem. 2005 Jan 13;48(1):163-70.

PMID:
15634010
19.

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
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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