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Items: 1 to 20 of 99

1.

Discovery of 6-substituted indole-3-glyoxylamides as lead antiprion agents with enhanced cell line activity, improved microsomal stability and low toxicity.

Thompson MJ, Louth JC, Ferrara S, Jackson MP, Sorrell FJ, Cochrane EJ, Gever J, Baxendale S, Silber BM, Roehl HH, Chen B.

Eur J Med Chem. 2011 Sep;46(9):4125-32. doi: 10.1016/j.ejmech.2011.06.013. Epub 2011 Jun 17.

PMID:
21726921
2.

Structure-activity relationship refinement and further assessment of indole-3-glyoxylamides as a lead series against prion disease.

Thompson MJ, Louth JC, Ferrara S, Sorrell FJ, Irving BJ, Cochrane EJ, Meijer AJ, Chen B.

ChemMedChem. 2011 Jan 3;6(1):115-30. doi: 10.1002/cmdc.201000383.

PMID:
21154498
3.

Design, synthesis, and structure-activity relationship of indole-3-glyoxylamide libraries possessing highly potent activity in a cell line model of prion disease.

Thompson MJ, Borsenberger V, Louth JC, Judd KE, Chen B.

J Med Chem. 2009 Dec 10;52(23):7503-11. doi: 10.1021/jm900920x.

PMID:
19842664
4.

Improved 2,4-diarylthiazole-based antiprion agents: switching the sense of the amide group at C5 leads to an increase in potency.

Thompson MJ, Louth JC, Greenwood GK, Sorrell FJ, Knight SG, Adams NB, Chen B.

ChemMedChem. 2010 Sep 3;5(9):1476-88. doi: 10.1002/cmdc.201000217.

PMID:
20635376
5.

An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer.

Colley HE, Muthana M, Danson SJ, Jackson LV, Brett ML, Harrison J, Coole SF, Mason DP, Jennings LR, Wong M, Tulasi V, Norman D, Lockey PM, Williams L, Dossetter AG, Griffen EJ, Thompson MJ.

J Med Chem. 2015 Dec 10;58(23):9309-33. doi: 10.1021/acs.jmedchem.5b01312. Epub 2015 Dec 1.

PMID:
26580420
6.

Design, synthesis, and biological evaluation of indole-2-carboxamides: a promising class of antituberculosis agents.

Kondreddi RR, Jiricek J, Rao SP, Lakshminarayana SB, Camacho LR, Rao R, Herve M, Bifani P, Ma NL, Kuhen K, Goh A, Chatterjee AK, Dick T, Diagana TT, Manjunatha UH, Smith PW.

J Med Chem. 2013 Nov 14;56(21):8849-59. doi: 10.1021/jm4012774. Epub 2013 Oct 22.

PMID:
24090347
7.

Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases.

Nishiguchi GA, Atallah G, Bellamacina C, Burger MT, Ding Y, Feucht PH, Garcia PD, Han W, Klivansky L, Lindvall M.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6366-9. doi: 10.1016/j.bmcl.2011.08.105. Epub 2011 Sep 10.

PMID:
21945284
8.
9.

Synthesis and structure activity relationships of schweinfurthin indoles.

Kodet JG, Beutler JA, Wiemer DF.

Bioorg Med Chem. 2014 Apr 15;22(8):2542-52. doi: 10.1016/j.bmc.2014.02.043. Epub 2014 Mar 6.

10.

Chemical genetics-based discovery of indole derivatives as HCV NS5B polymerase inhibitors.

Jin G, Lee S, Choi M, Son S, Kim GW, Oh JW, Lee C, Lee K.

Eur J Med Chem. 2014 Mar 21;75:413-25. doi: 10.1016/j.ejmech.2014.01.062. Epub 2014 Jan 31.

PMID:
24561671
11.

Discovery of 2-aminothiazoles as potent antiprion compounds.

Ghaemmaghami S, May BC, Renslo AR, Prusiner SB.

J Virol. 2010 Apr;84(7):3408-12. doi: 10.1128/JVI.02145-09. Epub 2009 Dec 23.

12.

Tyrosine kinase inhibitors. 6. Structure-activity relationships among N- and 3-substituted 2,2'-diselenobis(1H-indoles) for inhibition of protein tyrosine kinases and comparative in vitro and in vivo studies against selected sulfur congeners.

Showalter HD, Sercel AD, Leja BM, Wolfangel CD, Ambroso LA, Elliott WL, Fry DW, Kraker AJ, Howard CT, Lu GH, Moore CW, Nelson JM, Roberts BJ, Vincent PW, Denny WA, Thompson AM.

J Med Chem. 1997 Feb 14;40(4):413-26.

PMID:
9046331
13.

Preliminary SAR on indole-3-carbinol and related fragments reveals a novel anticancer lead compound against resistant glioblastoma cells.

Sherer C, Tolaymat I, Rowther F, Warr T, Snape TJ.

Bioorg Med Chem Lett. 2017 Apr 1;27(7):1561-1565. doi: 10.1016/j.bmcl.2017.02.033. Epub 2017 Feb 17.

PMID:
28256372
14.

Discovery, design, and synthesis of indole-based EZH2 inhibitors.

Gehling VS, Vaswani RG, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Dakin LA, Cook AS, Gagnon A, Harmange JC, Audia JE, Cummings RT, Normant E, Trojer P, Albrecht BK.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3644-9. doi: 10.1016/j.bmcl.2015.06.056. Epub 2015 Jun 19.

PMID:
26189078
15.

Indole- and indolizine-glyoxylamides displaying cytotoxicity against multidrug resistant cancer cell lines.

James DA, Koya K, Li H, Liang G, Xia Z, Ying W, Wu Y, Sun L.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1784-7. doi: 10.1016/j.bmcl.2008.02.029. Epub 2008 Feb 16.

PMID:
18308566
16.

The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.

Reid M, Carlyle I, Caulfield WL, Clarkson TR, Cusick F, Epemolu O, Gilfillan R, Goodwin R, Jaap D, O'Donnell EC, Presland J, Rankovic Z, Spinks D, Spinks G, Thomson AM, Thomson F, Strain J, Wishart G.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3713-6. doi: 10.1016/j.bmcl.2010.04.085. Epub 2010 Apr 24.

PMID:
20471831
17.

Similar structure-activity relationships of quinoline derivatives for antiprion and antimalarial effects.

Klingenstein R, Melnyk P, Leliveld SR, Ryckebusch A, Korth C.

J Med Chem. 2006 Aug 24;49(17):5300-8.

PMID:
16913719
18.

Structure-activity relationship of 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole analogues as 5-HT(6) receptor agonists.

Mattsson C, Svensson P, Boettcher H, Sonesson C.

Eur J Med Chem. 2013 May;63:578-88. doi: 10.1016/j.ejmech.2013.03.006. Epub 2013 Mar 14.

PMID:
23542166
19.

Novel indole-2-carboxamide compounds are potent broad-spectrum antivirals active against western equine encephalitis virus in vivo.

Delekta PC, Dobry CJ, Sindac JA, Barraza SJ, Blakely PK, Xiang J, Kirchhoff PD, Keep RF, Irani DN, Larsen SD, Miller DJ.

J Virol. 2014 Oct;88(19):11199-214. doi: 10.1128/JVI.01671-14. Epub 2014 Jul 16.

20.

Discovery of bisindolyl-substituted cycloalkane-anellated indoles as novel class of antibacterial agents against S. aureus and MRSA.

El-Sayed MT, Suzen S, Altanlar N, Ohlsen K, Hilgeroth A.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):218-21. doi: 10.1016/j.bmcl.2015.10.085. Epub 2015 Oct 29.

PMID:
26590101

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