Rigoreau LJ - Search Results

1

Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase.

Hollick JJ, Rigoreau LJ, Cano-Soumillac C, Cockcroft X, Curtin NJ, Frigerio M, Golding BT, Guiard S, Hardcastle IR, Hickson I, Hummersone MG, Menear KA, Martin NM, Matthews I, Newell DR, Ord R, Richardson CJ, Smith GC, Griffin RJ. Hollick JJ, et al. Among authors: rigoreau lj. J Med Chem. 2007 Apr 19;50(8):1958-72. doi: 10.1021/jm061121y. Epub 2007 Mar 20. J Med Chem. 2007. PMID: 17371003

2

Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035).

Stockley M, Clegg W, Fontana G, Golding BT, Martin N, Rigoreau LJ, Smith GC, Griffin RJ. Stockley M, et al. Among authors: rigoreau lj. Bioorg Med Chem Lett. 2001 Nov 5;11(21):2837-41. doi: 10.1016/s0960-894x(01)00537-6. Bioorg Med Chem Lett. 2001. PMID: 11597411

3

2,6-disubstituted pyran-4-one and thiopyran-4-one inhibitors of DNA-Dependent protein kinase (DNA-PK).

Hollick JJ, Golding BT, Hardcastle IR, Martin N, Richardson C, Rigoreau LJ, Smith GC, Griffin RJ. Hollick JJ, et al. Among authors: rigoreau lj. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3083-6. doi: 10.1016/s0960-894x(03)00652-8. Bioorg Med Chem Lett. 2003. PMID: 12941339

4

Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries.

Leahy JJ, Golding BT, Griffin RJ, Hardcastle IR, Richardson C, Rigoreau L, Smith GC. Leahy JJ, et al. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7. doi: 10.1016/j.bmcl.2004.09.060. Bioorg Med Chem Lett. 2004. PMID: 15546735

5

Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro.

Griffin RJ, Fontana G, Golding BT, Guiard S, Hardcastle IR, Leahy JJ, Martin N, Richardson C, Rigoreau L, Stockley M, Smith GC. Griffin RJ, et al. J Med Chem. 2005 Jan 27;48(2):569-85. doi: 10.1021/jm049526a. J Med Chem. 2005. PMID: 15658870

6

Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach.

Hardcastle IR, Cockcroft X, Curtin NJ, El-Murr MD, Leahy JJ, Stockley M, Golding BT, Rigoreau L, Richardson C, Smith GC, Griffin RJ. Hardcastle IR, et al. J Med Chem. 2005 Dec 1;48(24):7829-46. doi: 10.1021/jm050444b. J Med Chem. 2005. PMID: 16302822

7

Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion.

Golding SE, Rosenberg E, Valerie N, Hussaini I, Frigerio M, Cockcroft XF, Chong WY, Hummersone M, Rigoreau L, Menear KA, O'Connor MJ, Povirk LF, van Meter T, Valerie K. Golding SE, et al. Mol Cancer Ther. 2009 Oct;8(10):2894-902. doi: 10.1158/1535-7163.MCT-09-0519. Epub 2009 Oct 6. Mol Cancer Ther. 2009. PMID: 19808981 Free PMC article.

8

Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.

Caldwell JJ, Welsh EJ, Matijssen C, Anderson VE, Antoni L, Boxall K, Urban F, Hayes A, Raynaud FI, Rigoreau LJ, Raynham T, Aherne GW, Pearl LH, Oliver AW, Garrett MD, Collins I. Caldwell JJ, et al. Among authors: rigoreau lj. J Med Chem. 2011 Jan 27;54(2):580-90. doi: 10.1021/jm101150b. Epub 2010 Dec 27. J Med Chem. 2011. PMID: 21186793

9

Synthesis and structure-activity relationships for 1-(4-(piperidin-1-ylsulfonyl)phenyl)pyrrolidin-2-ones as novel non-carboxylate inhibitors of the aldo-keto reductase enzyme AKR1C3.

Heinrich DM, Flanagan JU, Jamieson SM, Silva S, Rigoreau LJ, Trivier E, Raynham T, Turnbull AP, Denny WA. Heinrich DM, et al. Among authors: rigoreau lj. Eur J Med Chem. 2013 Apr;62:738-44. doi: 10.1016/j.ejmech.2013.01.047. Epub 2013 Feb 9. Eur J Med Chem. 2013. PMID: 23454516

10

Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3).

Flanagan JU, Atwell GJ, Heinrich DM, Brooke DG, Silva S, Rigoreau LJ, Trivier E, Turnbull AP, Raynham T, Jamieson SM, Denny WA. Flanagan JU, et al. Among authors: rigoreau lj. Bioorg Med Chem. 2014 Feb 1;22(3):967-77. doi: 10.1016/j.bmc.2013.12.050. Epub 2014 Jan 2. Bioorg Med Chem. 2014. PMID: 24411201

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