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Items: 1 to 50 of 528

1.

Transcriptional changes in response to ketamine ester-analogs SN 35210 and SN 35563 in the rat brain.

Jacobson GM, Voss LJ, Klockars A, Bird S, Dimitrov I, Denny WA, Olszewski PK, Sleigh JW, Harvey MG.

BMC Genomics. 2019 Apr 11;20(1):281. doi: 10.1186/s12864-019-5649-6.

2.

Synthesis and biological evaluation of solubilized sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.

Giddens AC, Gamage SA, Kendall JD, Lee WJ, Baguley BC, Buchanan CM, Jamieson SMF, Dickson JMJ, Shepherd PR, Denny WA, Rewcastle GW.

Bioorg Med Chem. 2019 Apr 15;27(8):1529-1545. doi: 10.1016/j.bmc.2019.02.050. Epub 2019 Feb 25.

PMID:
30850264
3.

3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel.

Sutherland HS, Tong AST, Choi PJ, Blaser A, Conole D, Franzblau SG, Lotlikar MU, Cooper CB, Upton AM, Denny WA, Palmer BD.

Bioorg Med Chem. 2019 Apr 1;27(7):1292-1307. doi: 10.1016/j.bmc.2019.02.026. Epub 2019 Feb 15.

4.

Ketamine esters and amides as short-acting anaesthetics: Structure-activity relationships for the side-chain.

Dimitrov IV, Harvey MG, Voss LJ, Sleigh JW, Bickerdike MJ, Denny WA.

Bioorg Med Chem. 2019 Apr 1;27(7):1226-1231. doi: 10.1016/j.bmc.2019.02.010. Epub 2019 Feb 5.

PMID:
30792105
5.

Structure-activity relationships for unit C pyridyl analogues of the tuberculosis drug bedaquiline.

Blaser A, Sutherland HS, Tong AST, Choi PJ, Conole D, Franzblau SG, Cooper CB, Upton AM, Lotlikar M, Denny WA, Palmer BD.

Bioorg Med Chem. 2019 Apr 1;27(7):1283-1291. doi: 10.1016/j.bmc.2019.02.025. Epub 2019 Feb 15.

6.

Synthesis and Evaluation of Imidazo[1,2-a]pyridine Analogues of the ZSTK474 Class of Phosphatidylinositol 3-Kinase Inhibitors.

Gamage SA, Spicer JA, Tsang KY, O'Connor PD, Flanagan JU, Lee WJ, Dickson JMJ, Shepherd PR, Denny WA, Rewcastle GW.

Chem Asian J. 2019 Apr 15;14(8):1249-1261. doi: 10.1002/asia.201801762. Epub 2019 Mar 12.

PMID:
30714356
7.

Synthesis and Microtubule-Destabilizing Activity of N-Cyclopropyl-4-((3,4-dihydroquinolin-1(2H)-yl)sulfonyl)benzamide and its Analogs.

Field JJ, Singh AJ, Sinha S, Rowe MR, Denny WA, Brooke DG, Miller JH.

Chem Asian J. 2019 Apr 15;14(8):1151-1157. doi: 10.1002/asia.201801313. Epub 2018 Nov 14.

PMID:
30311418
8.

High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds.

Wang J, Gong GQ, Zhou Y, Lee WJ, Buchanan CM, Denny WA, Rewcastle GW, Kendall JD, Dickson JMJ, Flanagan JU, Shepherd PR, Yang DH, Wang MW.

Acta Pharmacol Sin. 2018 Nov;39(11):1816-1822. doi: 10.1038/s41401-018-0057-z. Epub 2018 Jul 10.

PMID:
29991713
9.

An SAR study of hydroxy-trifluoromethylpyrazolines as inhibitors of Orai1-mediated store operated Ca2+ entry in MDA-MB-231 breast cancer cells using a convenient Fluorescence Imaging Plate Reader assay.

Stevenson RJ, Azimi I, Flanagan JU, Inserra M, Vetter I, Monteith GR, Denny WA.

Bioorg Med Chem. 2018 Jul 23;26(12):3406-3413. doi: 10.1016/j.bmc.2018.05.012. Epub 2018 May 9.

PMID:
29776832
10.

A mitochondria-selective near-infrared-emitting fluorescent dye for cellular imaging studies.

Choi P, Noguchi K, Ishiyama M, Denny WA, Jose J.

Bioorg Med Chem Lett. 2018 Jun 15;28(11):2013-2017. doi: 10.1016/j.bmcl.2018.05.001. Epub 2018 May 3.

PMID:
29731365
11.

Inhibition of strigolactone receptors by N-phenylanthranilic acid derivatives: Structural and functional insights.

Hamiaux C, Drummond RSM, Luo Z, Lee HW, Sharma P, Janssen BJ, Perry NB, Denny WA, Snowden KC.

J Biol Chem. 2018 Apr 27;293(17):6530-6543. doi: 10.1074/jbc.RA117.001154. Epub 2018 Mar 9.

12.

Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles.

Sutherland HS, Tong AST, Choi PJ, Conole D, Blaser A, Franzblau SG, Cooper CB, Upton AM, Lotlikar MU, Denny WA, Palmer BD.

Bioorg Med Chem. 2018 May 1;26(8):1797-1809. doi: 10.1016/j.bmc.2018.02.026. Epub 2018 Feb 20.

13.

Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis.

Thompson AM, O'Connor PD, Marshall AJ, Blaser A, Yardley V, Maes L, Gupta S, Launay D, Braillard S, Chatelain E, Wan B, Franzblau SG, Ma Z, Cooper CB, Denny WA.

J Med Chem. 2018 Mar 22;61(6):2329-2352. doi: 10.1021/acs.jmedchem.7b01581. Epub 2018 Mar 6.

14.

Investigation into Improving the Aqueous Solubility of the Thieno[2,3-b]pyridine Anti-Proliferative Agents.

Zafar A, Pilkington LI, Haverkate NA, van Rensburg M, Leung E, Kumara S, Denny WA, Barker D, Alsuraifi A, Hoskins C, Reynisson J.

Molecules. 2018 Jan 11;23(1). pii: E145. doi: 10.3390/molecules23010145.

15.

Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.

Thompson AM, Bonnet M, Lee HH, Franzblau SG, Wan B, Wong GS, Cooper CB, Denny WA.

ACS Med Chem Lett. 2017 Nov 13;8(12):1275-1280. doi: 10.1021/acsmedchemlett.7b00356. eCollection 2017 Dec 14.

16.

Assessment of a pretomanid analogue library for African trypanosomiasis: Hit-to-lead studies on 6-substituted 2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine 8-oxides.

Thompson AM, Marshall AJ, Maes L, Yarlett N, Bacchi CJ, Gaukel E, Wring SA, Launay D, Braillard S, Chatelain E, Mowbray CE, Denny WA.

Bioorg Med Chem Lett. 2018 Jan 15;28(2):207-213. doi: 10.1016/j.bmcl.2017.10.067. Epub 2017 Oct 27.

17.

Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units.

Choi PJ, Sutherland HS, Tong AST, Blaser A, Franzblau SG, Cooper CB, Lotlikar MU, Upton AM, Guillemont J, Motte M, Queguiner L, Andries K, Van den Broeck W, Denny WA, Palmer BD.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5190-5196. doi: 10.1016/j.bmcl.2017.10.042. Epub 2017 Oct 20.

18.

6-Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis.

Tong AST, Choi PJ, Blaser A, Sutherland HS, Tsang SKY, Guillemont J, Motte M, Cooper CB, Andries K, Van den Broeck W, Franzblau SG, Upton AM, Denny WA, Palmer BD, Conole D.

ACS Med Chem Lett. 2017 Sep 22;8(10):1019-1024. doi: 10.1021/acsmedchemlett.7b00196. eCollection 2017 Oct 12.

19.

Synthesis and biological evaluation of sulfonamide analogues of the phosphatidylinositol 3-kinase inhibitor ZSTK474.

Gamage SA, Giddens AC, Tsang KY, Flanagan JU, Kendall JD, Lee WJ, Baguley BC, Buchanan CM, Jamieson SMF, Shepherd PR, Denny WA, Rewcastle GW.

Bioorg Med Chem. 2017 Oct 15;25(20):5859-5874. doi: 10.1016/j.bmc.2017.09.025. Epub 2017 Sep 20.

PMID:
28958845
20.

Substituted arylsulphonamides as inhibitors of perforin-mediated lysis.

Spicer JA, Miller CK, O'Connor PD, Jose J, Huttunen KM, Jaiswal JK, Denny WA, Akhlaghi H, Browne KA, Trapani JA.

Eur J Med Chem. 2017 Sep 8;137:139-155. doi: 10.1016/j.ejmech.2017.05.048. Epub 2017 May 26.

21.

Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors.

Rewcastle GW, Kolekar S, Buchanan CM, Gamage SA, Giddens AC, Tsang KY, Kendall JD, Singh R, Lee WJ, Smith GC, Han W, Matthews DJ, Denny WA, Shepherd PR, Jamieson SMF.

Oncotarget. 2017 Jul 18;8(29):47725-47740. doi: 10.18632/oncotarget.17730.

22.

Combining properties of different classes of PI3Kα inhibitors to understand the molecular features that confer selectivity.

Gong GQ, Kendall JD, Dickson JMJ, Rewcastle GW, Buchanan CM, Denny WA, Shepherd PR, Flanagan JU.

Biochem J. 2017 Jun 26;474(13):2261-2276. doi: 10.1042/BCJ20161098.

PMID:
28526744
23.

6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]thiazoles: Facile synthesis and comparative appraisal against tuberculosis and neglected tropical diseases.

Thompson AM, Blaser A, Palmer BD, Anderson RF, Shinde SS, Launay D, Chatelain E, Maes L, Franzblau SG, Wan B, Wang Y, Ma Z, Denny WA.

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2583-2589. doi: 10.1016/j.bmcl.2017.03.069. Epub 2017 Mar 27.

PMID:
28462832
24.

7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1-b][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis.

Thompson AM, O'Connor PD, Marshall AJ, Yardley V, Maes L, Gupta S, Launay D, Braillard S, Chatelain E, Franzblau SG, Wan B, Wang Y, Ma Z, Cooper CB, Denny WA.

J Med Chem. 2017 May 25;60(10):4212-4233. doi: 10.1021/acs.jmedchem.7b00034. Epub 2017 May 11.

25.

Recent developments in anticancer drug delivery using cell penetrating and tumor targeting peptides.

Dissanayake S, Denny WA, Gamage S, Sarojini V.

J Control Release. 2017 Mar 28;250:62-76. doi: 10.1016/j.jconrel.2017.02.006. Epub 2017 Feb 4. Review.

PMID:
28167286
26.

Benzenesulphonamide inhibitors of the cytolytic protein perforin.

Spicer JA, Miller CK, O'Connor PD, Jose J, Huttunen KM, Jaiswal JK, Denny WA, Akhlaghi H, Browne KA, Trapani JA.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):1050-1054. doi: 10.1016/j.bmcl.2016.12.057. Epub 2016 Dec 23.

27.

Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110α-selective PI3 kinase inhibitors.

Kendall JD, Giddens AC, Tsang KY, Marshall ES, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Jamieson SMF, Rewcastle GW, Baguley BC, Denny WA, Shepherd PR.

Bioorg Med Chem Lett. 2017 Jan 15;27(2):187-190. doi: 10.1016/j.bmcl.2016.11.078. Epub 2016 Nov 25.

PMID:
27923617
28.

Effect of common and experimental anti-tuberculosis treatments on Mycobacterium tuberculosis growing as biofilms.

Dalton JP, Uy B, Phummarin N, Copp BR, Denny WA, Swift S, Wiles S.

PeerJ. 2016 Nov 22;4:e2717. eCollection 2016.

29.

Homobivalent Conjugation Increases the Allosteric Effect of 9-aminoacridine at the α1-Adrenergic Receptors.

Campbell AP, Wakelin LP, Denny WA, Finch AM.

Mol Pharmacol. 2017 Feb;91(2):135-144. doi: 10.1124/mol.116.105874. Epub 2016 Nov 30.

PMID:
27903755
30.

Evaluation of known and novel inhibitors of Orai1-mediated store operated Ca2+ entry in MDA-MB-231 breast cancer cells using a Fluorescence Imaging Plate Reader assay.

Azimi I, Flanagan JU, Stevenson RJ, Inserra M, Vetter I, Monteith GR, Denny WA.

Bioorg Med Chem. 2017 Jan 1;25(1):440-449. doi: 10.1016/j.bmc.2016.11.007. Epub 2016 Nov 7.

PMID:
27856238
31.

Screening of anti-mycobacterial compounds in a naturally infected zebrafish larvae model.

Dalton JP, Uy B, Okuda KS, Hall CJ, Denny WA, Crosier PS, Swift S, Wiles S.

J Antimicrob Chemother. 2017 Feb;72(2):421-427. doi: 10.1093/jac/dkw421. Epub 2016 Oct 24.

PMID:
27798206
32.

Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.

Smaill JB, Gonzales AJ, Spicer JA, Lee H, Reed JE, Sexton K, Althaus IW, Zhu T, Black SL, Blaser A, Denny WA, Ellis PA, Fakhoury S, Harvey PJ, Hook K, McCarthy FO, Palmer BD, Rivault F, Schlosser K, Ellis T, Thompson AM, Trachet E, Winters RT, Tecle H, Bridges A.

J Med Chem. 2016 Sep 8;59(17):8103-24. doi: 10.1021/acs.jmedchem.6b00883. Epub 2016 Aug 22.

PMID:
27491023
33.

Systemic and Brain Pharmacokinetics of Perforin Inhibitor Prodrugs.

Gynther M, Pickering DS, Spicer JA, Denny WA, Huttunen KM.

Mol Pharm. 2016 Jul 5;13(7):2484-91. doi: 10.1021/acs.molpharmaceut.6b00217. Epub 2016 Jun 13.

PMID:
27266990
34.

A Selective and Slowly Reversible Inhibitor of l-Type Amino Acid Transporter 1 (LAT1) Potentiates Antiproliferative Drug Efficacy in Cancer Cells.

Huttunen KM, Gynther M, Huttunen J, Puris E, Spicer JA, Denny WA.

J Med Chem. 2016 Jun 23;59(12):5740-51. doi: 10.1021/acs.jmedchem.6b00190. Epub 2016 Jun 8.

PMID:
27253989
35.

Microtubule-stabilizing properties of the avocado-derived toxins (+)-(R)-persin and (+)-(R)-tetrahydropersin in cancer cells and activity of related synthetic analogs.

Field JJ, Kanakkanthara A, Brooke DG, Sinha S, Pillai SD, Denny WA, Butt AJ, Miller JH.

Invest New Drugs. 2016 Jun;34(3):277-89. doi: 10.1007/s10637-016-0341-z. Epub 2016 Mar 12.

PMID:
26968704
36.

Evidence that phospholipase C is involved in the antitumour action of NSC768313, a new thieno[2,3-b]pyridine derivative.

Reynisson J, Jaiswal JK, Barker D, D'mello SA, Denny WA, Baguley BC, Leung EY.

Cancer Cell Int. 2016 Mar 10;16:18. doi: 10.1186/s12935-016-0293-6. eCollection 2016.

37.

Repositioning Antitubercular 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazoles for Neglected Tropical Diseases: Structure-Activity Studies on a Preclinical Candidate for Visceral Leishmaniasis.

Thompson AM, O'Connor PD, Blaser A, Yardley V, Maes L, Gupta S, Launay D, Martin D, Franzblau SG, Wan B, Wang Y, Ma Z, Denny WA.

J Med Chem. 2016 Mar 24;59(6):2530-50. doi: 10.1021/acs.jmedchem.5b01699. Epub 2016 Mar 8.

38.

Synthesis and cytotoxicity of thieno[2,3-b]quinoline-2-carboxamide and cycloalkyl[b]thieno[3,2-e]pyridine-2-carboxamide derivatives.

Leung E, Pilkington LI, van Rensburg M, Jeon CY, Song M, Arabshahi HJ, De Zoysa GH, Sarojini V, Denny WA, Reynisson J, Barker D.

Bioorg Med Chem. 2016 Mar 1;24(5):1142-54. doi: 10.1016/j.bmc.2016.01.047. Epub 2016 Jan 27.

PMID:
26853836
39.

A quinazoline-based HDAC inhibitor affects gene expression pathways involved in cholesterol biosynthesis and mevalonate in prostate cancer cells.

Lin Z, Bishop KS, Sutherland H, Marlow G, Murray P, Denny WA, Ferguson LR.

Mol Biosyst. 2016 Mar;12(3):839-49. doi: 10.1039/c5mb00554j.

PMID:
26759180
40.

Diarylthiophenes as inhibitors of the pore-forming protein perforin.

Miller CK, Huttunen KM, Denny WA, Jaiswal JK, Ciccone A, Browne KA, Trapani JA, Spicer JA.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):355-360. doi: 10.1016/j.bmcl.2015.12.003. Epub 2015 Dec 7.

41.

L-Type amino acid transporter 1 (lat1)-mediated targeted delivery of perforin inhibitors.

Huttunen KM, Huttunen J, Aufderhaar I, Gynther M, Denny WA, Spicer JA.

Int J Pharm. 2016 Feb 10;498(1-2):205-16. doi: 10.1016/j.ijpharm.2015.12.034. Epub 2015 Dec 15.

PMID:
26705152
42.

Biarylmethoxy 2-nitroimidazooxazine antituberculosis agents: Effects of proximal ring substitution and linker reversal on metabolism and efficacy.

Thompson AM, Blaser A, Palmer BD, Franzblau SG, Wan B, Wang Y, Ma Z, Denny WA.

Bioorg Med Chem Lett. 2015 Sep 15;25(18):3804-9. doi: 10.1016/j.bmcl.2015.07.084. Epub 2015 Jul 28.

PMID:
26253632
43.

Corrigendum: Repurposing the Chemical Scaffold of the Anti-Arthritic Drug Lobenzarit to Target Tryptophan Biosynthesis in Mycobacterium tuberculosis.

Evans GL, Gamage SA, Bulloch EM, Baker EN, Denny WA, Lott JS.

Chembiochem. 2015 Mar 23;16(5):706. doi: 10.1002/cbic.201500098. Epub 2015 Mar 11. No abstract available.

PMID:
26177917
44.

COMMENTARY. Pre-emptive Nutrition: Refining the Targets of Drugs Targeted to Colorectal Cancer.

Ferguson LR, Denny WA.

Curr Cancer Drug Targets. 2015;15(3):173-5.

PMID:
25986644
45.

Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: synthesis, biological evaluation and molecular modelling.

Marshall AJ, Lill CL, Chao M, Kolekar SV, Lee WJ, Marshall ES, Baguley BC, Shepherd PR, Denny WA, Flanagan JU, Rewcastle GW.

Bioorg Med Chem. 2015 Jul 1;23(13):3796-808. doi: 10.1016/j.bmc.2015.03.073. Epub 2015 Apr 4.

PMID:
25890698
46.

Synthesis and structure-activity relationships for extended side chain analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824).

Palmer BD, Sutherland HS, Blaser A, Kmentova I, Franzblau SG, Wan B, Wang Y, Ma Z, Denny WA, Thompson AM.

J Med Chem. 2015 Apr 9;58(7):3036-59. doi: 10.1021/jm501608q. Epub 2015 Mar 27.

PMID:
25781074
47.

Human α1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines.

Chen J, Campbell AP, Urmi KF, Wakelin LP, Denny WA, Griffith R, Finch AM.

Bioorg Med Chem. 2014 Nov 1;22(21):5910-6. doi: 10.1016/j.bmc.2014.09.017. Epub 2014 Sep 16.

PMID:
25288493
48.

Fragmentation of the quinoxaline N-oxide bond to the ˙OH radical upon one-electron bioreduction.

Yadav P, Marshall AJ, Reynisson J, Denny WA, Hay MP, Anderson RF.

Chem Commun (Camb). 2014 Nov 18;50(89):13729-31. doi: 10.1039/c4cc05657d.

PMID:
25248989
49.

Comparison of hematin-targeting properties of pynacrine, an acridine analog of the benzonaphthyridine antimalarial pyronaridine.

Sereekhajornjaru N, Somboon C, Rattanajak R, Denny WA, Wilairat P, Auparakkitanon S.

Acta Trop. 2014 Dec;140:181-3. doi: 10.1016/j.actatropica.2014.09.002. Epub 2014 Sep 16.

PMID:
25220507
50.

The preclinical pharmacokinetic disposition of a series of perforin-inhibitors as potential immunosuppressive agents.

Bull MR, Spicer JA, Huttunen KM, Denny WA, Ciccone A, Browne KA, Trapani JA, Helsby NA.

Eur J Drug Metab Pharmacokinet. 2015 Dec;40(4):417-25. doi: 10.1007/s13318-014-0220-y. Epub 2014 Aug 26.

PMID:
25155444

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