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Results: 1 to 20 of 96

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
[PubMed - indexed for MEDLINE]
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
[PubMed - indexed for MEDLINE]
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
[PubMed - indexed for MEDLINE]
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
[PubMed - indexed for MEDLINE]
5.

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
[PubMed - indexed for MEDLINE]
6.

Procedure for identification and characterization of drugs efficient against mammalian prion: from a yeast-based antiprion drug screening assay to in vivo mouse models.

Voisset C, Saupe SJ, Galons H, Blondel M.

Infect Disord Drug Targets. 2009 Feb;9(1):31-9.

PMID:
19200013
[PubMed - indexed for MEDLINE]
7.

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
[PubMed - indexed for MEDLINE]
8.

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
[PubMed - indexed for MEDLINE]
9.

Virtual screening and structure-based discovery of indole acylguanidines as potent β-secretase (BACE1) inhibitors.

Zou Y, Li L, Chen W, Chen T, Ma L, Wang X, Xiong B, Xu Y, Shen J.

Molecules. 2013 May 16;18(5):5706-22. doi: 10.3390/molecules18055706.

PMID:
23681056
[PubMed - indexed for MEDLINE]
Free Article
10.

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
[PubMed - indexed for MEDLINE]
11.

Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.

Chen KX, Vibulbhan B, Yang W, Sannigrahi M, Velazquez F, Chan TY, Venkatraman S, Anilkumar GN, Zeng Q, Bennet F, Jiang Y, Lesburg CA, Duca J, Pinto P, Gavalas S, Huang Y, Wu W, Selyutin O, Agrawal S, Feld B, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG.

J Med Chem. 2012 Jan 26;55(2):754-65. doi: 10.1021/jm201258k. Epub 2012 Jan 6.

PMID:
22148957
[PubMed - indexed for MEDLINE]
12.

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
[PubMed - indexed for MEDLINE]
13.

I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.

Anilkumar GN, Lesburg CA, Selyutin O, Rosenblum SB, Zeng Q, Jiang Y, Chan TY, Pu H, Vaccaro H, Wang L, Bennett F, Chen KX, Duca J, Gavalas S, Huang Y, Pinto P, Sannigrahi M, Velazquez F, Venkatraman S, Vibulbhan B, Agrawal S, Butkiewicz N, Feld B, Ferrari E, He Z, Jiang CK, Palermo RE, McMonagle P, Huang HC, Shih NY, Njoroge G, Kozlowski JA.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5336-41. doi: 10.1016/j.bmcl.2011.07.021. Epub 2011 Jul 19.

PMID:
21840715
[PubMed - indexed for MEDLINE]
14.

N-substituted azaindoles as potent inhibitors of Cdc7 kinase.

Bryan MC, Falsey JR, Frohn M, Reichelt A, Yao G, Bartberger MD, Bailis JM, Zalameda L, Miguel TS, Doherty EM, Allen JG.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2056-60. doi: 10.1016/j.bmcl.2013.02.007. Epub 2013 Feb 13.

PMID:
23481650
[PubMed - indexed for MEDLINE]
15.

Indole RSK inhibitors. Part 1: discovery and initial SAR.

Boyer SJ, Burke J, Guo X, Kirrane TM, Snow RJ, Zhang Y, Sarko C, Soleymanzadeh L, Swinamer A, Westbrook J, Dicapua F, Padyana A, Cogan D, Gao A, Xiong Z, Madwed JB, Kashem M, Kugler S, O'Neill MM.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):733-7. doi: 10.1016/j.bmcl.2011.10.030. Epub 2011 Oct 14.

PMID:
22100312
[PubMed - indexed for MEDLINE]
16.

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
[PubMed - indexed for MEDLINE]
17.

Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.

Dai Y, Guo Y, Guo J, Pease LJ, Li J, Marcotte PA, Glaser KB, Tapang P, Albert DH, Richardson PL, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Jun 2;13(11):1897-901.

PMID:
12749893
[PubMed - indexed for MEDLINE]
18.

2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists.

Kher S, Lake K, Sircar I, Pannala M, Bakir F, Zapf J, Xu K, Zhang SH, Liu J, Morera L, Sakurai N, Jack R, Cheng JF.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4442-6. Epub 2007 Jun 10.

PMID:
17587573
[PubMed - indexed for MEDLINE]
19.

Quinols as novel therapeutic agents. 2.(1) 4-(1-Arylsulfonylindol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-ones and related agents as potent and selective antitumor agents.

Berry JM, Bradshaw TD, Fichtner I, Ren R, Schwalbe CH, Wells G, Chew EH, Stevens MF, Westwell AD.

J Med Chem. 2005 Jan 27;48(2):639-44.

PMID:
15658878
[PubMed - indexed for MEDLINE]
20.

Potent 1,3-disubstituted-9H-pyrido[3,4-b]indoles as new lead compounds in antifilarial chemotherapy.

Srivastava SK, Agarwal A, Chauhan PM, Agarwal SK, Bhaduri AP, Singh SN, Fatima N, Chatterjee RK.

J Med Chem. 1999 May 6;42(9):1667-72.

PMID:
10229635
[PubMed - indexed for MEDLINE]

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