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Items: 1 to 50 of 68

1.

Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.

Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang LZ, Wong AC, Noble MEM, Wedge SR, Cano C.

Eur J Med Chem. 2019 Sep 15;178:530-543. doi: 10.1016/j.ejmech.2019.05.057. Epub 2019 May 25.

PMID:
31212132
2.

FragLites-Minimal, Halogenated Fragments Displaying Pharmacophore Doublets. An Efficient Approach to Druggability Assessment and Hit Generation.

Wood DJ, Lopez-Fernandez JD, Knight LE, Al-Khawaldeh I, Gai C, Lin S, Martin MP, Miller DC, Cano C, Endicott JA, Hardcastle IR, Noble MEM, Waring MJ.

J Med Chem. 2019 Apr 11;62(7):3741-3752. doi: 10.1021/acs.jmedchem.9b00304. Epub 2019 Mar 26.

PMID:
30860382
3.

Recent advances in CDK inhibitors for cancer therapy.

Heptinstall AB, Adiyasa I, Cano C, Hardcastle IR.

Future Med Chem. 2018 Jun 1;10(11):1369-1388. doi: 10.4155/fmc-2017-0246. Epub 2018 May 30. Review.

PMID:
29846081
4.

Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach.

Miller DC, Martin MP, Adhikari S, Brennan A, Endicott JA, Golding BT, Hardcastle IR, Heptinstall A, Hobson S, Jennings C, Molyneux L, Ng Y, Wedge SR, Noble MEM, Cano C.

Org Biomol Chem. 2018 Mar 14;16(11):1843-1850. doi: 10.1039/c8ob00099a.

5.

Human Toxicity Caused by Indole and Indazole Carboxylate Synthetic Cannabinoid Receptor Agonists: From Horizon Scanning to Notification.

Hill SL, Dunn M, Cano C, Harnor SJ, Hardcastle IR, Grundlingh J, Dargan PI, Wood DM, Tucker S, Bartram T, Thomas SHL.

Clin Chem. 2018 Feb;64(2):346-354. doi: 10.1373/clinchem.2017.275867. Epub 2017 Oct 16.

PMID:
29038156
6.

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.

Coxon CR, Anscombe E, Harnor SJ, Martin MP, Carbain B, Golding BT, Hardcastle IR, Harlow LK, Korolchuk S, Matheson CJ, Newell DR, Noble ME, Sivaprakasam M, Tudhope SJ, Turner DM, Wang LZ, Wedge SR, Wong C, Griffin RJ, Endicott JA, Cano C.

J Med Chem. 2017 Mar 9;60(5):1746-1767. doi: 10.1021/acs.jmedchem.6b01254. Epub 2017 Feb 14.

7.

Structure-guided design of purine-based probes for selective Nek2 inhibition.

Coxon CR, Wong C, Bayliss R, Boxall K, Carr KH, Fry AM, Hardcastle IR, Matheson CJ, Newell DR, Sivaprakasam M, Thomas H, Turner D, Yeoh S, Wang LZ, Griffin RJ, Golding BT, Cano C.

Oncotarget. 2017 Mar 21;8(12):19089-19124. doi: 10.18632/oncotarget.13249.

8.

Combined PI3K and CDK2 inhibition induces cell death and enhances in vivo antitumour activity in colorectal cancer.

Beale G, Haagensen EJ, Thomas HD, Wang LZ, Revill CH, Payne SL, Golding BT, Hardcastle IR, Newell DR, Griffin RJ, Cano C.

Br J Cancer. 2016 Sep 6;115(6):682-90. doi: 10.1038/bjc.2016.238. Epub 2016 Aug 16.

9.

High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors.

Myers SM, Bawn RH, Bisset LC, Blackburn TJ, Cottyn B, Molyneux L, Wong AC, Cano C, Clegg W, Harrington RW, Leung H, Rigoreau L, Vidot S, Golding BT, Griffin RJ, Hammonds T, Newell DR, Hardcastle IR.

ACS Comb Sci. 2016 Aug 8;18(8):444-55. doi: 10.1021/acscombsci.5b00155. Epub 2016 Jul 20.

PMID:
27400250
10.

TP53 mutant MDM2-amplified cell lines selected for resistance to MDM2-p53 binding antagonists retain sensitivity to ionizing radiation.

Drummond CJ, Esfandiari A, Liu J, Lu X, Hutton C, Jackson J, Bennaceur K, Xu Q, Makimanejavali AR, Del Bello F, Piergentili A, Newell DR, Hardcastle IR, Griffin RJ, Lunec J.

Oncotarget. 2016 Jul 19;7(29):46203-46218. doi: 10.18632/oncotarget.10073.

11.

Aryne generation vs. Truce-Smiles and fries rearrangements during the Kobayashi fragmentation reaction: a new bi-aryl synthesis.

Rasheed OK, Hardcastle IR, Raftery J, Quayle P.

Org Biomol Chem. 2015 Aug 7;13(29):8048-52. doi: 10.1039/c5ob01239b. Epub 2015 Jul 1.

PMID:
26126413
12.

Small-molecule MDM2-p53 inhibitors: recent advances.

Zhang B, Golding BT, Hardcastle IR.

Future Med Chem. 2015;7(5):631-45. doi: 10.4155/fmc.15.13. Review.

PMID:
25921402
13.

Searching for Dual Inhibitors of the MDM2-p53 and MDMX-p53 Protein-Protein Interaction by a Scaffold-Hopping Approach.

Zaytsev A, Dodd B, Magnani M, Ghiron C, Golding BT, Griffin RJ, Liu J, Lu X, Micco I, Newell DR, Padova A, Robertson G, Lunec J, Hardcastle IR.

Chem Biol Drug Des. 2015 Aug;86(2):180-9. doi: 10.1111/cbdd.12474. Epub 2014 Dec 19.

PMID:
25388787
14.

Trifluoroacetic acid in 2,2,2-trifluoroethanol facilitates S(N)Ar reactions of heterocycles with arylamines.

Carbain B, Coxon CR, Lebraud H, Elliott KJ, Matheson CJ, Meschini E, Roberts AR, Turner DM, Wong C, Cano C, Griffin RJ, Hardcastle IR, Golding BT.

Chemistry. 2014 Feb 17;20(8):2311-7. doi: 10.1002/chem.201304336. Epub 2014 Jan 23.

PMID:
24458729
15.

8-Substituted O(6)-cyclohexylmethylguanine CDK2 inhibitors: using structure-based inhibitor design to optimize an alternative binding mode.

Carbain B, Paterson DJ, Anscombe E, Campbell AJ, Cano C, Echalier A, Endicott JA, Golding BT, Haggerty K, Hardcastle IR, Jewsbury PJ, Newell DR, Noble ME, Roche C, Wang LZ, Griffin RJ.

J Med Chem. 2014 Jan 9;57(1):56-70. doi: 10.1021/jm401555v. Epub 2013 Dec 23.

PMID:
24304238
16.

Model system for irreversible inhibition of Nek2: thiol addition to ethynylpurines and related substituted heterocycles.

Lebraud H, Coxon CR, Archard VS, Bawn CM, Carbain B, Matheson CJ, Turner DM, Cano C, Griffin RJ, Hardcastle IR, Baisch U, Harrington RW, Golding BT.

Org Biomol Chem. 2014 Jan 7;12(1):141-8. doi: 10.1039/c3ob41806e. Epub 2013 Nov 8.

PMID:
24213855
18.

1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.

Cano C, Saravanan K, Bailey C, Bardos J, Curtin NJ, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Menear KA, Newell DR, Richardson CJ, Shea K, Smith GC, Thommes P, Ting A, Griffin RJ.

J Med Chem. 2013 Aug 22;56(16):6386-401. doi: 10.1021/jm400915j. Epub 2013 Aug 1.

PMID:
23855836
19.

Trifluoroethanol solvent facilitates selective N-7 methylation of purines.

Lebraud H, Cano C, Carbain B, Hardcastle IR, Harrington RW, Griffin RJ, Golding BT.

Org Biomol Chem. 2013 Mar 21;11(11):1874-8. doi: 10.1039/c3ob27473j. Epub 2013 Feb 4.

PMID:
23381666
20.

Characterisation of a Tip60 specific inhibitor, NU9056, in prostate cancer.

Coffey K, Blackburn TJ, Cook S, Golding BT, Griffin RJ, Hardcastle IR, Hewitt L, Huberman K, McNeill HV, Newell DR, Roche C, Ryan-Munden CA, Watson A, Robson CN.

PLoS One. 2012;7(10):e45539. doi: 10.1371/journal.pone.0045539. Epub 2012 Oct 8.

21.

Potent enantioselective inhibition of DNA-dependent protein kinase (DNA-PK) by atropisomeric chromenone derivatives.

Clapham KM, Rennison T, Jones G, Craven F, Bardos J, Golding BT, Griffin RJ, Haggerty K, Hardcastle IR, Thommes P, Ting A, Cano C.

Org Biomol Chem. 2012 Sep 7;10(33):6747-57. doi: 10.1039/c2ob26035b. Epub 2012 Jul 19.

PMID:
22814419
22.

MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones.

Watson AF, Liu J, Bennaceur K, Drummond CJ, Endicott JA, Golding BT, Griffin RJ, Haggerty K, Lu X, McDonnell JM, Newell DR, Noble ME, Revill CH, Riedinger C, Xu Q, Zhao Y, Lunec J, Hardcastle IR.

Bioorg Med Chem Lett. 2011 Oct 1;21(19):5916-9. doi: 10.1016/j.bmcl.2011.07.084. Epub 2011 Aug 9.

PMID:
21875801
23.

Versatile synthesis of functionalised dibenzothiophenes via Suzuki coupling and microwave-assisted ring closure.

Rodriguez-Aristegui S, Clapham KM, Barrett L, Cano C, Desage-El Murr M, Griffin RJ, Hardcastle IR, Payne SL, Rennison T, Richardson C, Golding BT.

Org Biomol Chem. 2011 Sep 7;9(17):6066-74. doi: 10.1039/c1ob05282a. Epub 2011 Jul 12.

PMID:
21748189
24.

Preclinical in vitro and in vivo evaluation of the potent and specific cyclin-dependent kinase 2 inhibitor NU6102 and a water soluble prodrug NU6301.

Thomas HD, Wang LZ, Roche C, Bentley J, Cheng Y, Hardcastle IR, Golding BT, Griffin RJ, Curtin NJ, Newell DR.

Eur J Cancer. 2011 Sep;47(13):2052-9. doi: 10.1016/j.ejca.2011.04.008. Epub 2011 May 12.

PMID:
21570822
25.

Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.

Hardcastle IR, Liu J, Valeur E, Watson A, Ahmed SU, Blackburn TJ, Bennaceur K, Clegg W, Drummond C, Endicott JA, Golding BT, Griffin RJ, Gruber J, Haggerty K, Harrington RW, Hutton C, Kemp S, Lu X, McDonnell JM, Newell DR, Noble ME, Payne SL, Revill CH, Riedinger C, Xu Q, Lunec J.

J Med Chem. 2011 Mar 10;54(5):1233-43. doi: 10.1021/jm1011929. Epub 2011 Feb 11.

PMID:
21314128
26.

Understanding small-molecule binding to MDM2: insights into structural effects of isoindolinone inhibitors from NMR spectroscopy.

Riedinger C, Noble ME, Wright DJ, Mulks F, Hardcastle IR, Endicott JA, McDonnell JM.

Chem Biol Drug Des. 2011 May;77(5):301-8. doi: 10.1111/j.1747-0285.2011.01091.x. Epub 2011 Mar 1.

PMID:
21244642
27.

DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain.

Clapham KM, Bardos J, Finlay MR, Golding BT, Griffen EJ, Griffin RJ, Hardcastle IR, Menear KA, Ting A, Turner P, Young GL, Cano C.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):966-70. doi: 10.1016/j.bmcl.2010.12.047. Epub 2010 Dec 13.

PMID:
21216595
28.

DNA-dependent protein kinase (DNA-PK) inhibitors. Synthesis and biological activity of quinolin-4-one and pyridopyrimidin-4-one surrogates for the chromen-4-one chemotype.

Cano C, Barbeau OR, Bailey C, Cockcroft XL, Curtin NJ, Duggan H, Frigerio M, Golding BT, Hardcastle IR, Hummersone MG, Knights C, Menear KA, Newell DR, Richardson CJ, Smith GC, Spittle B, Griffin RJ.

J Med Chem. 2010 Dec 23;53(24):8498-507. doi: 10.1021/jm100608j. Epub 2010 Nov 16.

PMID:
21080722
29.

Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors.

Payne SL, Rodriguez-Aristegui S, Bardos J, Cano C, Golding BT, Hardcastle IR, Peacock M, Parveen N, Griffin RJ.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3649-53. doi: 10.1016/j.bmcl.2010.04.102. Epub 2010 May 14.

PMID:
20472428
30.

Atropisomeric 8-arylchromen-4-ones exhibit enantioselective inhibition of the DNA-dependent protein kinase (DNA-PK).

Cano C, Golding BT, Haggerty K, Hardcastle IR, Peacock M, Griffin RJ.

Org Biomol Chem. 2010 Apr 21;8(8):1922-8. doi: 10.1039/b926245h.

PMID:
20449499
31.

Synthesis of sulfonamide-based kinase inhibitors from sulfonates by exploiting the abrogated SN2 reactivity of 2,2,2-trifluoroethoxysulfonates.

Wong C, Griffin RJ, Hardcastle IR, Northen JS, Wang LZ, Golding BT.

Org Biomol Chem. 2010 May 21;8(10):2457-64. doi: 10.1039/b922717b. Epub 2010 Mar 24.

PMID:
20448906
32.

Synthesis and biological evaluation of 5-substituted O4-alkylpyrimidines as CDK2 inhibitors.

Marchetti F, Cano C, Curtin NJ, Golding BT, Griffin RJ, Haggerty K, Newell DR, Parsons RJ, Payne SL, Wang LZ, Hardcastle IR.

Org Biomol Chem. 2010 May 21;8(10):2397-407. doi: 10.1039/b925481a. Epub 2010 Mar 18.

PMID:
20448898
33.

Analysis of chemical shift changes reveals the binding modes of isoindolinone inhibitors of the MDM2-p53 interaction.

Riedinger C, Endicott JA, Kemp SJ, Smyth LA, Watson A, Valeur E, Golding BT, Griffin RJ, Hardcastle IR, Noble ME, McDonnell JM.

J Am Chem Soc. 2008 Nov 26;130(47):16038-44. doi: 10.1021/ja8062088.

PMID:
18959403
34.

8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).

Desage-El Murr M, Cano C, Golding BT, Hardcastle IR, Hummersome M, Frigerio M, Curtin NJ, Menear K, Richardson C, Smith GC, Griffin RJ.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4885-90. doi: 10.1016/j.bmcl.2008.07.066. Epub 2008 Jul 20.

PMID:
18678488
35.

Quinolinone and pyridopyrimidinone inhibitors of DNA-dependent protein kinase.

Barbeau OR, Cano-Soumillac C, Griffin RJ, Hardcastle IR, Smith GC, Richardson C, Clegg W, Harrington RW, Golding BT.

Org Biomol Chem. 2007 Aug 21;5(16):2670-7.

PMID:
18019542
36.

Structure-based design of 2-arylamino-4-cyclohexylmethoxy-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinase 2.

Marchetti F, Sayle KL, Bentley J, Clegg W, Curtin NJ, Endicott JA, Golding BT, Griffin RJ, Haggerty K, Harrington RW, Mesguiche V, Newell DR, Noble ME, Parsons RJ, Pratt DJ, Wang LZ, Hardcastle IR.

Org Biomol Chem. 2007 May 21;5(10):1577-85. Epub 2007 Apr 23.

PMID:
17571187
37.

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.

J Med Chem. 2007 Apr 19;50(8):1958-72. Epub 2007 Mar 20.

PMID:
17371003
38.
39.

A new strategy for the synthesis of taurine derivatives using the 'safety-catch' principle for the protection of sulfonic acids.

Seeberger S, Griffin RJ, Hardcastle IR, Golding BT.

Org Biomol Chem. 2007 Jan 7;5(1):132-8. Epub 2006 Nov 24.

PMID:
17164917
40.

Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold.

Hardcastle IR, Ahmed SU, Atkins H, Farnie G, Golding BT, Griffin RJ, Guyenne S, Hutton C, Källblad P, Kemp SJ, Kitching MS, Newell DR, Norbedo S, Northen JS, Reid RJ, Saravanan K, Willems HM, Lunec J.

J Med Chem. 2006 Oct 19;49(21):6209-21.

PMID:
17034127
41.

Searching for cyclin-dependent kinase inhibitors using a new variant of the cope elimination.

Griffin RJ, Henderson A, Curtin NJ, Echalier A, Endicott JA, Hardcastle IR, Newell DR, Noble ME, Wang LZ, Golding BT.

J Am Chem Soc. 2006 May 10;128(18):6012-3.

PMID:
16669651
42.

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.

J Med Chem. 2005 Dec 1;48(24):7829-46.

PMID:
16302822
43.

An evaluation of the ability of pifithrin-alpha and -beta to inhibit p53 function in two wild-type p53 human tumor cell lines.

Walton MI, Wilson SC, Hardcastle IR, Mirza AR, Workman P.

Mol Cancer Ther. 2005 Sep;4(9):1369-77.

44.

Potentiation of paclitaxel-induced apoptosis by the novel cyclin-dependent kinase inhibitor NU6140: a possible role for survivin down-regulation.

Pennati M, Campbell AJ, Curto M, Binda M, Cheng Y, Wang LZ, Curtin N, Golding BT, Griffin RJ, Hardcastle IR, Henderson A, Zaffaroni N, Newell DR.

Mol Cancer Ther. 2005 Sep;4(9):1328-37.

45.

Isoindolinone-based inhibitors of the MDM2-p53 protein-protein interaction.

Hardcastle IR, Ahmed SU, Atkins H, Calvert AH, Curtin NJ, Farnie G, Golding BT, Griffin RJ, Guyenne S, Hutton C, Källblad P, Kemp SJ, Kitching MS, Newell DR, Norbedo S, Northen JS, Reid RJ, Saravanan K, Willems HM, Lunec J.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1515-20.

PMID:
15713419
46.

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.

J Med Chem. 2005 Jan 27;48(2):569-85.

PMID:
15658870
47.

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.

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7.

PMID:
15546735
48.

N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2.

Hardcastle IR, Arris CE, Bentley J, Boyle FT, Chen Y, Curtin NJ, Endicott JA, Gibson AE, Golding BT, Griffin RJ, Jewsbury P, Menyerol J, Mesguiche V, Newell DR, Noble ME, Pratt DJ, Wang LZ, Whitfield HJ.

J Med Chem. 2004 Jul 15;47(15):3710-22.

PMID:
15239650
49.

Facilitation of addition-elimination reactions in pyrimidines and purines using trifluoroacetic acid in trifluoroethanol.

Whitfield HJ, Griffin RJ, Hardcastle IR, Henderson A, Meneyrol J, Mesguiche V, Sayle KL, Golding BT.

Chem Commun (Camb). 2003 Nov 21;(22):2802-3.

PMID:
14651112
50.

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.

Bioorg Med Chem Lett. 2003 Sep 15;13(18):3083-6.

PMID:
12941339

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