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Items: 1 to 50 of 60

1.

The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain.

Brown AD, Bagal SK, Blackwell P, Blakemore DC, Brown B, Bungay PJ, Corless M, Crawforth J, Fengas D, Fenwick DR, Gray V, Kemp M, Klute W, Malet Sanz L, Miller D, Murata Y, Payne CE, Skerratt S, Stevens EB, Warmus JS.

Bioorg Med Chem. 2019 Jan 1;27(1):230-239. doi: 10.1016/j.bmc.2018.12.002. Epub 2018 Dec 4.

PMID:
30538065
2.

Photochemical Homologation for the Preparation of Aliphatic Aldehydes in Flow.

Chen Y, Leonardi M, Dingwall P, Labes R, Pasau P, Blakemore DC, Ley SV.

J Org Chem. 2018 Nov 29. doi: 10.1021/acs.joc.8b02721. [Epub ahead of print]

PMID:
30444967
3.

Heterocyclic Allylsulfones as Latent Heteroaryl Nucleophiles in Palladium-Catalyzed Cross-Coupling Reactions.

Markovic T, Murray PRD, Rocke BN, Shavnya A, Blakemore DC, Willis MC.

J Am Chem Soc. 2018 Nov 21;140(46):15916-15923. doi: 10.1021/jacs.8b09595. Epub 2018 Nov 9.

PMID:
30412397
4.

Three-Component Assembly of Multiply Substituted Homoallylic Alcohols and Amines Using a Flow Chemistry Photoreactor.

Chen Y, Blakemore DC, Pasau P, Ley SV.

Org Lett. 2018 Oct 19;20(20):6569-6572. doi: 10.1021/acs.orglett.8b02907. Epub 2018 Oct 1.

PMID:
30270627
5.

C-H functionalisation of aldehydes using light generated, non-stabilised diazo compounds in flow.

Dingwall P, Greb A, Crespin LNS, Labes R, Musio B, Poh JS, Pasau P, Blakemore DC, Ley SV.

Chem Commun (Camb). 2018 Oct 16;54(83):11685-11688. doi: 10.1039/c8cc06202a.

PMID:
30203830
6.

Fine-Tuning Mybl2 Is Required for Proper Mesenchymal-to-Epithelial Transition during Somatic Reprogramming.

Ward C, Volpe G, Cauchy P, Ptasinska A, Almaghrabi R, Blakemore D, Nafria M, Kestner D, Frampton J, Murphy G, Buganim Y, Kaji K, García P.

Cell Rep. 2018 Aug 7;24(6):1496-1511.e8. doi: 10.1016/j.celrep.2018.07.026.

7.

MYBL2 Supports DNA Double Strand Break Repair in Hematopoietic Stem Cells.

Bayley R, Blakemore D, Cancian L, Dumon S, Volpe G, Ward C, Almaghrabi R, Gujar J, Reeve N, Raghavan M, Higgs MR, Stewart GS, Petermann E, García P.

Cancer Res. 2018 Oct 15;78(20):5767-5779. doi: 10.1158/0008-5472.CAN-18-0273. Epub 2018 Aug 6.

PMID:
30082276
8.

Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain.

Bagal SK, Andrews M, Bechle BM, Bian J, Bilsland J, Blakemore DC, Braganza JF, Bungay PJ, Corbett MS, Cronin CN, Cui JJ, Dias R, Flanagan NJ, Greasley SE, Grimley R, James K, Johnson E, Kitching L, Kraus ML, McAlpine I, Nagata A, Ninkovic S, Omoto K, Scales S, Skerratt SE, Sun J, Tran-Dubé M, Waldron GJ, Wang F, Warmus JS.

J Med Chem. 2018 Aug 9;61(15):6779-6800. doi: 10.1021/acs.jmedchem.8b00633. Epub 2018 Jul 27.

PMID:
29944371
9.

Correction to "Catalyst Selection Facilitates the Use of Heterocyclic Sulfinates as General Nucleophilic Coupling Partners in Palladium-Catalyzed Coupling Reactions".

Markovic T, Rocke BN, Blakemore DC, Mascitti V, Willis MC.

Org Lett. 2018 May 18;20(10):3148-3149. doi: 10.1021/acs.orglett.8b01120. Epub 2018 May 9. No abstract available.

PMID:
29741085
10.

Discovery of Allosteric, Potent, Subtype Selective, and Peripherally Restricted TrkA Kinase Inhibitors.

Bagal SK, Omoto K, Blakemore DC, Bungay PJ, Bilsland JG, Clarke PJ, Corbett MS, Cronin CN, Cui JJ, Dias R, Flanagan NJ, Greasley SE, Grimley R, Johnson E, Fengas D, Kitching L, Kraus ML, McAlpine I, Nagata A, Waldron GJ, Warmus JS.

J Med Chem. 2018 May 3. doi: 10.1021/acs.jmedchem.8b00280. [Epub ahead of print]

PMID:
29672039
11.

Organic synthesis provides opportunities to transform drug discovery.

Blakemore DC, Castro L, Churcher I, Rees DC, Thomas AW, Wilson DM, Wood A.

Nat Chem. 2018 Apr;10(4):383-394. doi: 10.1038/s41557-018-0021-z. Epub 2018 Mar 22. Review.

PMID:
29568051
12.

Visible-Light-Mediated Annulation of Electron-Rich Alkenes and Nitrogen-Centered Radicals from N-Sulfonylallylamines: Construction of Chloromethylated Pyrrolidine Derivatives.

Crespin LNS, Greb A, Blakemore DC, Ley SV.

J Org Chem. 2017 Dec 15;82(24):13093-13108. doi: 10.1021/acs.joc.7b02146. Epub 2017 Nov 22.

PMID:
29121471
13.

A Versatile Route to Unstable Diazo Compounds via Oxadiazolines and their Use in Aryl-Alkyl Cross-Coupling Reactions.

Greb A, Poh JS, Greed S, Battilocchio C, Pasau P, Blakemore DC, Ley SV.

Angew Chem Int Ed Engl. 2017 Dec 22;56(52):16602-16605. doi: 10.1002/anie.201710445. Epub 2017 Dec 5.

14.

Catalyst Selection Facilitates the Use of Heterocyclic Sulfinates as General Nucleophilic Coupling Partners in Palladium-Catalyzed Coupling Reactions.

Markovic T, Rocke BN, Blakemore DC, Mascitti V, Willis MC.

Org Lett. 2017 Nov 17;19(22):6033-6035. doi: 10.1021/acs.orglett.7b02944. Epub 2017 Oct 18. Erratum in: Org Lett. 2018 May 18;20(10 ):3148-3149.

PMID:
29043813
15.

Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes.

Storer RI, Pike A, Swain NA, Alexandrou AJ, Bechle BM, Blakemore DC, Brown AD, Castle NA, Corbett MS, Flanagan NJ, Fengas D, Johnson MS, Jones LH, Marron BE, Payne CE, Printzenhoff D, Rawson DJ, Rose CR, Ryckmans T, Sun J, Theile JW, Torella R, Tseng E, Warmus JS.

Bioorg Med Chem Lett. 2017 Nov 1;27(21):4805-4811. doi: 10.1016/j.bmcl.2017.09.056. Epub 2017 Sep 28.

PMID:
29029933
16.

Pyridine sulfinates as general nucleophilic coupling partners in palladium-catalyzed cross-coupling reactions with aryl halides.

Markovic T, Rocke BN, Blakemore DC, Mascitti V, Willis MC.

Chem Sci. 2017 Jun 1;8(6):4437-4442. doi: 10.1039/c7sc00675f. Epub 2017 Apr 28.

17.

Prognostic significance of high GFI1 expression in AML of normal karyotype and its association with a FLT3-ITD signature.

Volpe G, Walton DS, Grainger DE, Ward C, Cauchy P, Blakemore D, Coleman DJL, Cockerill PN, Garcia P, Frampton J.

Sci Rep. 2017 Sep 11;7(1):11148. doi: 10.1038/s41598-017-11718-8.

18.

Reductive Coupling of Acrylates with Ketones and Ketimines by a Nickel-Catalyzed Transfer-Hydrogenative Strategy.

Buxton CS, Blakemore DC, Bower JF.

Angew Chem Int Ed Engl. 2017 Oct 23;56(44):13824-13828. doi: 10.1002/anie.201707531. Epub 2017 Oct 4.

19.

Site-selective Suzuki-Miyaura coupling of heteroaryl halides - understanding the trends for pharmaceutically important classes.

Almond-Thynne J, Blakemore DC, Pryde DC, Spivey AC.

Chem Sci. 2017 Jan 1;8(1):40-62. doi: 10.1039/c6sc02118b. Epub 2016 Aug 9.

20.

Synthesis of 3-Substituted 2-Arylpyridines via Cu/Pd-Catalyzed Decarboxylative Cross-Coupling of Picolinic Acids with (Hetero)Aryl Halides.

Hackenberger D, Weber P, Blakemore DC, Goossen LJ.

J Org Chem. 2017 Apr 7;82(7):3917-3925. doi: 10.1021/acs.joc.7b00046. Epub 2017 Mar 16.

PMID:
28300402
21.

One-Pot Synthesis of α-Branched N-Acylamines via Titanium-Mediated Condensation of Amides, Aldehydes, and Organometallics.

Dai C, Genovino J, Bechle BM, Corbett MS, Huh CW, Rose CR, Sun J, Warmus JS, Blakemore DC.

Org Lett. 2017 Mar 3;19(5):1064-1067. doi: 10.1021/acs.orglett.7b00082. Epub 2017 Feb 15.

PMID:
28199125
22.

One-Pot Acid-Catalyzed Ring-Opening/Cyclization/Oxidation of Aziridines with N-Tosylhydrazones: Access to 1,2,4-Triazines.

Crespin L, Biancalana L, Morack T, Blakemore DC, Ley SV.

Org Lett. 2017 Mar 3;19(5):1084-1087. doi: 10.1021/acs.orglett.7b00101. Epub 2017 Feb 15.

23.

Fluorodecarboxylation for the Synthesis of Trifluoromethyl Aryl Ethers.

Zhang QW, Brusoe AT, Mascitti V, Hesp KD, Blakemore DC, Kohrt JT, Hartwig JF.

Angew Chem Int Ed Engl. 2016 Aug 8;55(33):9758-62. doi: 10.1002/anie.201604793. Epub 2016 Jul 7.

PMID:
27384710
24.

Modern advances in heterocyclic chemistry in drug discovery.

Taylor AP, Robinson RP, Fobian YM, Blakemore DC, Jones LH, Fadeyi O.

Org Biomol Chem. 2016 Jul 12;14(28):6611-37. doi: 10.1039/c6ob00936k. Review.

PMID:
27282396
25.

Synthesis of trifluoromethylated isoxazoles and their elaboration through inter- and intra-molecular C-H arylation.

Poh JS, García-Ruiz C, Zúñiga A, Meroni F, Blakemore DC, Browne DL, Ley SV.

Org Biomol Chem. 2016 Jul 7;14(25):5983-91. doi: 10.1039/c6ob00970k. Epub 2016 May 26.

PMID:
27225313
26.

Iterative reactions of transient boronic acids enable sequential C-C bond formation.

Battilocchio C, Feist F, Hafner A, Simon M, Tran DN, Allwood DM, Blakemore DC, Ley SV.

Nat Chem. 2016 Apr;8(4):360-7. doi: 10.1038/nchem.2439. Epub 2016 Feb 8.

PMID:
27001732
27.

Multidirectional Synthesis of Substituted Indazoles via Iridium-Catalyzed C-H Borylation.

Sadler SA, Hones AC, Roberts B, Blakemore D, Marder TB, Steel PG.

J Org Chem. 2015 May 15;80(10):5308-14. doi: 10.1021/acs.joc.5b00452. Epub 2015 May 1.

PMID:
25894824
28.

Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.

Rouquet G, Moore DE, Spain M, Allwood DM, Battilocchio C, Blakemore DC, Fish PV, Jenkinson S, Jessiman AS, Ley SV, McMurray G, Storer RI.

ACS Med Chem Lett. 2015 Jan 20;6(3):329-33. doi: 10.1021/ml500507v. eCollection 2015 Mar 12.

29.

Fluorine in drug design: a case study with fluoroanisoles.

Xing L, Blakemore DC, Narayanan A, Unwalla R, Lovering F, Denny RA, Zhou H, Bunnage ME.

ChemMedChem. 2015 Apr;10(4):715-26. doi: 10.1002/cmdc.201402555. Epub 2015 Mar 6.

PMID:
25755132
30.

The ortho-substituent effect on the Ag-catalysed decarboxylation of benzoic acids.

Grainger R, Cornella J, Blakemore DC, Larrosa I, Campanera JM.

Chemistry. 2014 Dec 8;20(50):16680-7. doi: 10.1002/chem.201402931. Epub 2014 Oct 21.

PMID:
25336158
31.

Regioselective preparation of saturated spirocyclic and ring-expanded fused pyrazoles.

Merchant RR, Allwood DM, Blakemore DC, Ley SV.

J Org Chem. 2014 Sep 19;79(18):8800-11. doi: 10.1021/jo501624t. Epub 2014 Aug 28.

PMID:
25148419
32.

Iridium-catalyzed C-H borylation of pyridines.

Sadler SA, Tajuddin H, Mkhalid IA, Batsanov AS, Albesa-Jove D, Cheung MS, Maxwell AC, Shukla L, Roberts B, Blakemore DC, Lin Z, Marder TB, Steel PG.

Org Biomol Chem. 2014 Oct 7;12(37):7318-27. doi: 10.1039/c4ob01565g.

PMID:
25116330
33.

Highly regioselective lithiation of pyridines bearing an oxetane unit by n-butyllithium.

Rouquet G, Blakemore DC, Ley SV.

Chem Commun (Camb). 2014 Aug 18;50(64):8908-11. doi: 10.1039/c4cc03766a.

PMID:
24969811
34.

Preparation of unsymmetrical ketones from tosylhydrazones and aromatic aldehydes via formyl C-H bond insertion.

Allwood DM, Blakemore DC, Ley SV.

Org Lett. 2014 Jun 6;16(11):3064-7. doi: 10.1021/ol5011714. Epub 2014 May 12.

PMID:
24819872
35.

On the synthesis of α-amino sulfoxides.

Rayner PJ, Gelardi G, O'Brien P, Horan RA, Blakemore DC.

Org Biomol Chem. 2014 Jun 7;12(21):3499-512. doi: 10.1039/c4ob00567h. Epub 2014 Apr 24.

PMID:
24759885
36.

The discovery of potent nonstructural protein 5A (NS5A) inhibitors with a unique resistance profile-Part 2.

Wakenhut F, Tran TD, Pickford C, Shaw S, Westby M, Smith-Burchnell C, Watson L, Paradowski M, Milbank J, Stonehouse D, Cheung K, Wybrow R, Daverio F, Crook S, Statham K, Leese D, Stead D, Adam F, Hay D, Roberts LR, Chiva JY, Nichols C, Blakemore DC, Goetz GH, Che Y, Gardner I, Dayal S, Pike A, Webster R, Pryde DC.

ChemMedChem. 2014 Jul;9(7):1387-96. doi: 10.1002/cmdc.201400046. Epub 2014 Apr 11.

PMID:
24729518
37.

The discovery of potent nonstructural protein 5A (NS5A) inhibitors with a unique resistance profile-Part 1.

Tran TD, Wakenhut F, Pickford C, Shaw S, Westby M, Smith-Burchnell C, Watson L, Paradowski M, Milbank J, Brimage RA, Halstead R, Glen R, Wilson CP, Adam F, Hay D, Chiva JY, Nichols C, Blakemore DC, Gardner I, Dayal S, Pike A, Webster R, Pryde DC.

ChemMedChem. 2014 Jul;9(7):1378-86. doi: 10.1002/cmdc.201400045. Epub 2014 Apr 11.

PMID:
24729513
38.

Metal-free coupling of saturated heterocyclic sulfonylhydrazones with boronic acids.

Allwood DM, Blakemore DC, Brown AD, Ley SV.

J Org Chem. 2014 Jan 3;79(1):328-38. doi: 10.1021/jo402526z. Epub 2013 Dec 10.

PMID:
24304206
39.

Asymmetric lithiation trapping of N-Boc heterocycles at temperatures above -78 °C.

Gelardi G, Barker G, O'Brien P, Blakemore DC.

Org Lett. 2013 Nov 1;15(21):5424-7. doi: 10.1021/ol402395j. Epub 2013 Oct 15.

PMID:
24180685
40.

Selection of a novel anti-nicotine vaccine: influence of antigen design on antibody function in mice.

Pryde DC, Jones LH, Gervais DP, Stead DR, Blakemore DC, Selby MD, Brown AD, Coe JW, Badland M, Beal DM, Glen R, Wharton Y, Miller GJ, White P, Zhang N, Benoit M, Robertson K, Merson JR, Davis HL, McCluskie MJ.

PLoS One. 2013 Oct 1;8(10):e76557. doi: 10.1371/journal.pone.0076557. eCollection 2013.

41.

Diastereoselective synthesis of β-heteroaryl syn-α-methyl-β-amino acid derivatives via a double chiral auxiliary approach.

Bian J, Blakemore D, Warmus JS, Sun J, Corbett M, Rose CR, Bechle BM.

Org Lett. 2013 Feb 1;15(3):562-5. doi: 10.1021/ol3033785. Epub 2013 Jan 23.

PMID:
23343056
42.

Dichotomous effects of exposure to bivalirudin in patients undergoing percutaneous coronary intervention on protease-activated receptor-mediated platelet activation.

Holinstat M, Colowick NE, Hudson WJ, Blakemore D, Chen Q, Hamm HE, Cleator JH.

J Thromb Thrombolysis. 2013 Feb;35(2):209-22. doi: 10.1007/s11239-012-0812-9.

43.

Weight loss and related behavior changes among lesbians.

Fogel S, Young L, Dietrich M, Blakemore D.

J Homosex. 2012;59(5):689-702. doi: 10.1080/00918369.2012.673937.

PMID:
22587359
44.

3T magnetic resonance imaging accurately depicts radiofrequency ablation zones in a blood-perfused bovine liver model.

Burns SK, Dodd GD 3rd, McManus LM, Cardan RA, Peng Q, Orsi MD, Head HW, Blakemore DL, Blume JD, Fullerton GD, Green TJ.

J Vasc Interv Radiol. 2012 Jun;23(6):801-8. doi: 10.1016/j.jvir.2012.01.076. Epub 2012 Mar 28.

PMID:
22459879
45.

Pentoxifylline lowers plasminogen activator inhibitor 1 levels in obese individuals: a pilot study.

Muldowney JA 3rd, Chen Q, Blakemore DL, Vaughan DE.

Angiology. 2012 Aug;63(6):429-34. doi: 10.1177/0003319712436755. Epub 2012 Feb 17.

PMID:
22345157
46.

Suboptimal inhibition of platelet cyclooxygenase-1 by aspirin in metabolic syndrome.

Smith JP, Haddad EV, Taylor MB, Oram D, Blakemore D, Chen Q, Boutaud O, Oates JA.

Hypertension. 2012 Mar;59(3):719-25. doi: 10.1161/HYPERTENSIONAHA.111.181404. Epub 2012 Feb 6.

47.

New lithium-zincate approaches for the selective functionalisation of pyrazine: direct dideprotozincation vs. nucleophilic alkylation.

Baillie SE, Blair VL, Blakemore DC, Hay D, Kennedy AR, Pryde DC, Hevia E.

Chem Commun (Camb). 2012 Feb 14;48(14):1985-7. doi: 10.1039/c2cc16959b. Epub 2012 Jan 11.

PMID:
22237409
48.

Circulating neuregulin-1β levels vary according to the angiographic severity of coronary artery disease and ischemia.

Geisberg CA, Wang G, Safa RN, Smith HM, Anderson B, Peng XY, Veerkamp B, Zhao DX, Blakemore D, Yu C, Sawyer DB.

Coron Artery Dis. 2011 Dec;22(8):577-82. doi: 10.1097/MCA.0b013e32834d3346.

49.

In vitro blood-perfused bovine liver model: a physiologic model for evaluation of the performance of radiofrequency ablation devices.

Orsi MD, Dodd GD 3rd, Cardan RA, Head HW, Burns SK, Blakemore D, Blume J, Green TJ.

J Vasc Interv Radiol. 2011 Oct;22(10):1478-83. doi: 10.1016/j.jvir.2011.06.013. Epub 2011 Jul 28.

PMID:
21802317
50.

Rapid access to α-alkoxy and α-amino acid derivatives through safe continuous-flow generation of diazoesters.

Bartrum HE, Blakemore DC, Moody CJ, Hayes CJ.

Chemistry. 2011 Aug 22;17(35):9586-9. doi: 10.1002/chem.201101590. Epub 2011 Jul 27. No abstract available.

PMID:
21796696

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