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Items: 1 to 50 of 172

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.

Photochemistry of 2-butenedial and 4-oxo-2-pentenal under atmospheric boundary layer conditions.

Newland MJ, Rea GJ, Thüner LP, Henderson AP, Golding BT, Rickard AR, Barnes I, Wenger J.

Phys Chem Chem Phys. 2019 Jan 21;21(3):1160-1171. doi: 10.1039/c8cp06437g. Epub 2019 Jan 8.

PMID:
30620029
3.

Hydrogen Sulfide: A Reagent for pH-Driven Bioinspired 1,2-Diol Mono-deoxygenation and Carbonyl Reduction in Water.

Barata-Vallejo S, Ferreri C, Golding BT, Chatgilialoglu C.

Org Lett. 2018 Jul 20;20(14):4290-4294. doi: 10.1021/acs.orglett.8b01713. Epub 2018 Jul 9.

PMID:
29985623
4.

The consequences of 'Brexit' for drug discovery and development, and the regulatory implications.

Golding BT, Waring MJ.

Expert Opin Drug Discov. 2018 Jul;13(7):583-585. doi: 10.1080/17460441.2018.1463215. Epub 2018 Apr 15. No abstract available.

PMID:
29634365
5.

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.

6.

Cooperative hydrogen bonds form a pseudocycle stabilizing an isolated complex of isocyanic acid with urea.

Mullaney JC, Medcraft C, Tew DP, Lewis-Borrell L, Golding BT, Walker NR, Legon AC.

Phys Chem Chem Phys. 2017 Sep 20;19(36):25080-25085. doi: 10.1039/c7cp04315e.

PMID:
28880033
7.

Conversion of cis-2-carboxycyclohexylacetyl-CoA in the downstream pathway of anaerobic naphthalene degradation.

Weyrauch P, Zaytsev AV, Stephan S, Kocks L, Schmitz OJ, Golding BT, Meckenstock RU.

Environ Microbiol. 2017 Jul;19(7):2819-2830. doi: 10.1111/1462-2920.13806. Epub 2017 Jul 3.

PMID:
28574200
8.

The impact of Brexit on British science: Also Sprach Zunderland.

Golding BT.

Future Med Chem. 2017 Mar;9(3):271-273. doi: 10.4155/fmc-2016-0245. Epub 2017 Feb 8. No abstract available.

PMID:
28176537
9.

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.

10.

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.

11.

A new tool for the chemical genetic investigation of the Plasmodium falciparum Pfnek-2 NIMA-related kinase.

Mitcheson DF, Bottrill AR, Carr K, Coxon CR, Cano C, Golding BT, Griffin RJ, Fry AM, Doerig C, Bayliss R, Tobin AB.

Malar J. 2016 Nov 7;15(1):535.

12.

COST Action CM1201 "Biomimetic Radical Chemistry": free radical chemistry successfully meets many disciplines.

Ferreri C, Golding BT, Jahn U, Ravanat JL.

Free Radic Res. 2016 Nov;50(sup1):S112-S128. Review.

PMID:
27750460
13.

New derivatives of the antimalarial drug Pyrimethamine in the control of melanoma tumor growth: an in vitro and in vivo study.

Tommasino C, Gambardella L, Buoncervello M, Griffin RJ, Golding BT, Alberton M, Macchia D, Spada M, Cerbelli B, d'Amati G, Malorni W, Gabriele L, Giammarioli AM.

J Exp Clin Cancer Res. 2016 Sep 6;35(1):137. doi: 10.1186/s13046-016-0409-9.

14.

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.

15.

Elucidating the Stereochemistry of Enzymatic Benzylsuccinate Synthesis with Chirally Labeled Toluene.

Seyhan D, Friedrich P, Szaleniec M, Hilberg M, Buckel W, Golding BT, Heider J.

Angew Chem Int Ed Engl. 2016 Sep 12;55(38):11664-7. doi: 10.1002/anie.201605197. Epub 2016 Aug 9.

PMID:
27503670
16.

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
17.

Synthesis and Biological Evaluation of N(2) -Substituted 2,4-Diamino-6-cyclohexylmethoxy-5-nitrosopyrimidines and Related 5-Cyano-NNO-azoxy Derivatives as Cyclin-Dependent Kinase 2 (CDK2) Inhibitors.

Cortese D, Chegaev K, Guglielmo S, Wang LZ, Golding BT, Cano C, Fruttero R.

ChemMedChem. 2016 Aug 19;11(16):1705-8. doi: 10.1002/cmdc.201600108. Epub 2016 Jun 29.

PMID:
27355194
18.

Design and synthesis of biphenyl and biphenyl ether inhibitors of sulfatases.

Reuillon T, Alhasan SF, Beale GS, Bertoli A, Brennan A, Cano C, Reeves HL, Newell DR, Golding BT, Miller DC, Griffin RJ.

Chem Sci. 2016 Apr 21;7(4):2821-2826. doi: 10.1039/c5sc03612g. Epub 2016 Jan 11.

19.

Anaerobic Microbial Degradation of Hydrocarbons: From Enzymatic Reactions to the Environment.

Rabus R, Boll M, Heider J, Meckenstock RU, Buckel W, Einsle O, Ermler U, Golding BT, Gunsalus RP, Kroneck PM, Krüger M, Lueders T, Martins BM, Musat F, Richnow HH, Schink B, Seifert J, Szaleniec M, Treude T, Ullmann GM, Vogt C, von Bergen M, Wilkes H.

J Mol Microbiol Biotechnol. 2016;26(1-3):5-28. doi: 10.1159/000443997. Epub 2016 Mar 10. Review.

20.

Structure and Function of 4-Hydroxyphenylacetate Decarboxylase and Its Cognate Activating Enzyme.

Selvaraj B, Buckel W, Golding BT, Ullmann GM, Martins BM.

J Mol Microbiol Biotechnol. 2016;26(1-3):76-91. doi: 10.1159/000440882. Epub 2016 Mar 10. Review.

PMID:
26959876
21.

Metabolism of Hydrocarbons in n-Alkane-Utilizing Anaerobic Bacteria.

Wilkes H, Buckel W, Golding BT, Rabus R.

J Mol Microbiol Biotechnol. 2016;26(1-3):138-51. doi: 10.1159/000442160. Epub 2016 Mar 10. Review.

PMID:
26959725
22.

Structure and Function of Benzylsuccinate Synthase and Related Fumarate-Adding Glycyl Radical Enzymes.

Heider J, Szaleniec M, Martins BM, Seyhan D, Buckel W, Golding BT.

J Mol Microbiol Biotechnol. 2016;26(1-3):29-44. doi: 10.1159/000441656. Epub 2016 Mar 10. Review.

PMID:
26959246
23.

Versatile transformations of hydrocarbons in anaerobic bacteria: substrate ranges and regio- and stereo-chemistry of activation reactions.

Jarling R, Kühner S, Basílio Janke E, Gruner A, Drozdowska M, Golding BT, Rabus R, Wilkes H.

Front Microbiol. 2015 Sep 7;6:880. doi: 10.3389/fmicb.2015.00880. eCollection 2015.

24.

1918 pandemic influenza virus and Streptococcus pneumoniae co-infection results in activation of coagulation and widespread pulmonary thrombosis in mice and humans.

Walters KA, D'Agnillo F, Sheng ZM, Kindrachuk J, Schwartzman LM, Kuestner RE, Chertow DS, Golding BT, Taubenberger JK, Kash JC.

J Pathol. 2016 Jan;238(1):85-97. doi: 10.1002/path.4638. Epub 2015 Oct 14.

25.

Identification and Characterization of an Irreversible Inhibitor of CDK2.

Anscombe E, Meschini E, Mora-Vidal R, Martin MP, Staunton D, Geitmann M, Danielson UH, Stanley WA, Wang LZ, Reuillon T, Golding BT, Cano C, Newell DR, Noble ME, Wedge SR, Endicott JA, Griffin RJ.

Chem Biol. 2015 Sep 17;22(9):1159-64. doi: 10.1016/j.chembiol.2015.07.018. Epub 2015 Aug 27.

26.

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
27.

Academic medicinal chemistry: no country for young men (or women)?

Golding BT.

Future Med Chem. 2015;7(5):549-51. doi: 10.4155/fmc.15.10. No abstract available.

28.

Regioselective sulfamoylation at low temperature enables concise syntheses of putative small molecule inhibitors of sulfatases.

Miller DC, Carbain B, Beale GS, Alhasan SF, Reeves HL, Baisch U, Newell DR, Golding BT, Griffin RJ.

Org Biomol Chem. 2015 May 14;13(18):5279-84. doi: 10.1039/c5ob00211g.

PMID:
25858034
29.

Non-enzymatic ribonucleotide reduction in the prebiotic context.

Dragičević I, Barić D, Kovačević B, Golding BT, Smith DM.

Chemistry. 2015 Apr 13;21(16):6132-43. doi: 10.1002/chem.201405741. Epub 2015 Mar 6.

PMID:
25754795
30.

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
31.

Anaerobic activation of p-cymene in denitrifying betaproteobacteria: methyl group hydroxylation versus addition to fumarate.

Strijkstra A, Trautwein K, Jarling R, Wöhlbrand L, Dörries M, Reinhardt R, Drozdowska M, Golding BT, Wilkes H, Rabus R.

Appl Environ Microbiol. 2014 Dec;80(24):7592-603. doi: 10.1128/AEM.02385-14. Epub 2014 Sep 26.

32.

Sir John Warcup Cornforth (1917-2013).

Golding BT, Buckel W.

Angew Chem Int Ed Engl. 2014 Apr 1;53(14):3546. doi: 10.1002/anie.201401077. Epub 2014 Mar 5. No abstract available.

PMID:
24599877
33.

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
34.

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
35.

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
37.

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
38.

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
39.

ATP-dependent/-independent enzymatic ring reductions involved in the anaerobic catabolism of naphthalene.

Eberlein C, Johannes J, Mouttaki H, Sadeghi M, Golding BT, Boll M, Meckenstock RU.

Environ Microbiol. 2013 Jun;15(6):1832-41. doi: 10.1111/1462-2920.12076. Epub 2013 Jan 22.

PMID:
23336264
40.

Mechanism-based design, synthesis and biological studies of N⁵-substituted tetrahydrofolate analogs as inhibitors of cobalamin-dependent methionine synthase and potential anticancer agents.

Zhang Z, Tian C, Zhou S, Wang W, Guo Y, Xia J, Liu Z, Wang B, Wang X, Golding BT, Griff RJ, Du Y, Liu J.

Eur J Med Chem. 2012 Dec;58:228-36. doi: 10.1016/j.ejmech.2012.09.027. Epub 2012 Oct 9.

PMID:
23124219
41.

Experimental study of hydrogen bonding potentially stabilizing the 5'-deoxyadenosyl radical from coenzyme B12.

Friedrich P, Baisch U, Harrington RW, Lyatuu F, Zhou K, Zelder F, McFarlane W, Buckel W, Golding BT.

Chemistry. 2012 Dec 7;18(50):16114-22. doi: 10.1002/chem.201201840. Epub 2012 Oct 18.

PMID:
23080006
42.

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.

43.

Hydrogen bonds guide the short-lived 5'-deoxyadenosyl radical to the place of action.

Buckel W, Friedrich P, Golding BT.

Angew Chem Int Ed Engl. 2012 Oct 1;51(40):9974-6. doi: 10.1002/anie.201205299. Epub 2012 Sep 3. No abstract available.

PMID:
22945861
44.

Efficacious N-protection of O-aryl sulfamates with 2,4-dimethoxybenzyl groups.

Reuillon T, Bertoli A, Griffin RJ, Miller DC, Golding BT.

Org Biomol Chem. 2012 Oct 7;10(37):7610-7. doi: 10.1039/c2ob26057c. Epub 2012 Aug 14.

PMID:
22893112
45.

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
46.

Revisiting the reaction of hydroxyl radicals with vicinal diols in water.

Jiang D, Barata-Vallejo S, Golding BT, Ferreri C, Chatgilialoglu C.

Org Biomol Chem. 2012 Feb 7;10(5):1102-7. doi: 10.1039/c1ob06538f. Epub 2011 Dec 14.

PMID:
22167177
47.

Stereochemical investigations reveal the mechanism of the bacterial activation of n-alkanes without oxygen.

Jarling R, Sadeghi M, Drozdowska M, Lahme S, Buckel W, Rabus R, Widdel F, Golding BT, Wilkes H.

Angew Chem Int Ed Engl. 2012 Feb 6;51(6):1334-8. doi: 10.1002/anie.201106055. Epub 2011 Nov 30. No abstract available.

PMID:
22127985
48.

Molecular hijacking of siroheme for the synthesis of heme and d1 heme.

Bali S, Lawrence AD, Lobo SA, Saraiva LM, Golding BT, Palmer DJ, Howard MJ, Ferguson SJ, Warren MJ.

Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18260-5. doi: 10.1073/pnas.1108228108. Epub 2011 Oct 3.

49.

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
50.

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

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