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Items: 1 to 50 of 96

1.

Radiosynthesis of [18F]-Labelled Pro-Nucleotides (ProTides).

Cavaliere A, Probst KC, Paisey SJ, Marshall C, Dheere AKH, Aigbirhio F, McGuigan C, Westwell AD.

Molecules. 2020 Feb 6;25(3). pii: E704. doi: 10.3390/molecules25030704.

2.

Structural modifications on CORM-3 lead to enhanced anti-angiogenic properties against triple-negative breast cancer cells.

Kourti M, Cai J, Jiang W, Westwell AD.

Med Chem. 2019 Dec 5. doi: 10.2174/1573406415666191206102452. [Epub ahead of print]

PMID:
31808392
3.

Polyfluoroaromatic stavudine (d4T) ProTides exhibit enhanced anti-HIV activity.

Kandil S, Pannecouque C, Chapman FM, Westwell AD, McGuigan C.

Bioorg Med Chem Lett. 2019 Dec 15;29(24):126721. doi: 10.1016/j.bmcl.2019.126721. Epub 2019 Oct 23.

PMID:
31679972
4.

The Anti-mycobacterial Activity of a Diterpenoid-Like Molecule Operates Through Nitrogen and Amino Acid Starvation.

Crusco A, Baptista R, Bhowmick S, Beckmann M, Mur LAJ, Westwell AD, Hoffmann KF.

Front Microbiol. 2019 Jun 25;10:1444. doi: 10.3389/fmicb.2019.01444. eCollection 2019.

5.

A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer.

Pertusati F, Ferla S, Bassetto M, Brancale A, Khandil S, Westwell AD, McGuigan C.

Eur J Med Chem. 2019 Oct 15;180:1-14. doi: 10.1016/j.ejmech.2019.07.001. Epub 2019 Jul 3.

PMID:
31288149
6.

Antischistosomal Properties of Sclareol and Its Heck-Coupled Derivatives: Design, Synthesis, Biological Evaluation, and Untargeted Metabolomics.

Crusco A, Whiteland H, Baptista R, Forde-Thomas JE, Beckmann M, Mur LAJ, Nash RJ, Westwell AD, Hoffmann KF.

ACS Infect Dis. 2019 Jul 12;5(7):1188-1199. doi: 10.1021/acsinfecdis.9b00034. Epub 2019 May 28.

PMID:
31083889
7.

New Quinoline-Based Heterocycles as Anticancer Agents Targeting Bcl-2.

Hamdy R, Elseginy SA, Ziedan NI, Jones AT, Westwell AD.

Molecules. 2019 Apr 2;24(7). pii: E1274. doi: 10.3390/molecules24071274.

8.

Emerging from the dark side: new therapeutic applications of scheduled psychoactive substances.

James E, Robertshaw TL, Westwell AD.

Future Med Chem. 2019 Feb 14. doi: 10.4155/fmc-2018-0447. [Epub ahead of print] No abstract available.

PMID:
30763121
9.

Discovery of deshydroxy bicalutamide derivatives as androgen receptor antagonists.

Kandil S, Lee KY, Davies L, Rizzo SA, Dart DA, Westwell AD.

Eur J Med Chem. 2019 Apr 1;167:49-60. doi: 10.1016/j.ejmech.2019.01.054. Epub 2019 Feb 2.

PMID:
30743097
10.

Corrigendum to "Gold nanoparticle conjugated Rad6 inhibitor induces cell death in triple negative breast cancer cells by inducing mitochondrial dysfunction and PARP-1 hyperactivation: Synthesis and characterization" [Nanomedicine 12 (3) (2016), 745-757].

Haynes B, Zhang Y, Liu F, Li J, Petit S, Kothayer H, Bao X, Westwell AD, Mao G, Shekhar MP.

Nanomedicine. 2019 Jun;18:426. doi: 10.1016/j.nano.2019.01.005. Epub 2019 Feb 3. No abstract available.

PMID:
30726707
11.

A framework for the development of effective anti-metastatic agents.

Anderson RL, Balasas T, Callaghan J, Coombes RC, Evans J, Hall JA, Kinrade S, Jones D, Jones PS, Jones R, Marshall JF, Panico MB, Shaw JA, Steeg PS, Sullivan M, Tong W, Westwell AD, Ritchie JWA; Cancer Research UK and Cancer Therapeutics CRC Australia Metastasis Working Group.

Nat Rev Clin Oncol. 2019 Mar;16(3):185-204. doi: 10.1038/s41571-018-0134-8.

PMID:
30514977
12.

Novel Trifluoromethylated Enobosarm Analogues with Potent Antiandrogenic Activity In Vitro and Tissue Selectivity In Vivo.

Dart DA, Kandil S, Tommasini-Ghelfi S, Serrano de Almeida G, Bevan CL, Jiang W, Westwell AD.

Mol Cancer Ther. 2018 Sep;17(9):1846-1858. doi: 10.1158/1535-7163.MCT-18-0037. Epub 2018 Jun 12.

13.

Design, synthesis and anthelmintic activity of 7-keto-sempervirol analogues.

Crusco A, Bordoni C, Chakroborty A, Whatley KCL, Whiteland H, Westwell AD, Hoffmann KF.

Eur J Med Chem. 2018 May 25;152:87-100. doi: 10.1016/j.ejmech.2018.04.032. Epub 2018 Apr 17.

14.

Fluorinated nucleosides as an important class of anticancer and antiviral agents.

Cavaliere A, Probst KC, Westwell AD, Slusarczyk M.

Future Med Chem. 2017 Oct;9(15):1809-1833. doi: 10.4155/fmc-2017-0095. Epub 2017 Sep 20. Review.

PMID:
28929804
15.

The discovery of new and more potent chloropyramine (C4) analogues for the potential treatment of invasive breast cancer.

Kandil S, Prencipe F, Jones S, Hiscox S, Westwell AD.

Chem Biol Drug Des. 2018 Jan;91(1):314-321. doi: 10.1111/cbdd.13083. Epub 2017 Aug 30.

PMID:
28816016
16.

RAD6 promotes DNA repair and stem cell signaling in ovarian cancer and is a promising therapeutic target to prevent and treat acquired chemoresistance.

Somasagara RR, Spencer SM, Tripathi K, Clark DW, Mani C, Madeira da Silva L, Scalici J, Kothayer H, Westwell AD, Rocconi RP, Palle K.

Oncogene. 2017 Nov 30;36(48):6680-6690. doi: 10.1038/onc.2017.279. Epub 2017 Aug 14.

17.

Pharmacologically directed strategies in academic anticancer drug discovery based on the European NCI compounds initiative.

Hendriks HR, Govaerts AS, Fichtner I, Burtles S, Westwell AD, Peters GJ.

Br J Cancer. 2017 Jul 11;117(2):195-202. doi: 10.1038/bjc.2017.167. Epub 2017 Jun 13.

18.

Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents.

Bassetto M, Ferla S, Giancotti G, Pertusati F, Westwell AD, Brancale A, McGuigan C.

Medchemcomm. 2017 May 26;8(7):1414-1420. doi: 10.1039/c7md00164a. eCollection 2017 Jul 1.

19.

Synthesis and evaluation of 5-(1H-indol-3-yl)-N-aryl-1,3,4-oxadiazol-2-amines as Bcl-2 inhibitory anticancer agents.

Hamdy R, Ziedan NI, Ali S, Bordoni C, El-Sadek M, Lashin E, Brancale A, Jones AT, Westwell AD.

Bioorg Med Chem Lett. 2017 Feb 15;27(4):1037-1040. doi: 10.1016/j.bmcl.2016.12.061. Epub 2016 Dec 27.

PMID:
28087272
20.

Virtual screening, SAR, and discovery of 5-(indole-3-yl)-2-[(2-nitrophenyl)amino] [1,3,4]-oxadiazole as a novel Bcl-2 inhibitor.

Ziedan NI, Hamdy R, Cavaliere A, Kourti M, Prencipe F, Brancale A, Jones AT, Westwell AD.

Chem Biol Drug Des. 2017 Jul;90(1):147-155. doi: 10.1111/cbdd.12936. Epub 2017 Feb 24.

PMID:
28067996
21.

The Role of BCA2 in the Endocytic Trafficking of EGFR and Significance as a Prognostic Biomarker in Cancer.

Wymant JM, Hiscox S, Westwell AD, Urbé S, Clague MJ, Jones AT.

J Cancer. 2016 Dec 9;7(15):2388-2407. eCollection 2016.

22.

ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites.

Kandil S, Balzarini J, Rat S, Brancale A, Westwell AD, McGuigan C.

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5618-5623. doi: 10.1016/j.bmcl.2016.10.077. Epub 2016 Oct 27.

23.

Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety.

Ferla S, Bassetto M, Pertusati F, Kandil S, Westwell AD, Brancale A, McGuigan C.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3636-40. doi: 10.1016/j.bmcl.2016.06.001. Epub 2016 Jun 2.

PMID:
27301368
24.

Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.

Bassetto M, Ferla S, Pertusati F, Kandil S, Westwell AD, Brancale A, McGuigan C.

Eur J Med Chem. 2016 Aug 8;118:230-43. doi: 10.1016/j.ejmech.2016.04.052. Epub 2016 Apr 22.

25.

7-Substituted umbelliferone derivatives as androgen receptor antagonists for the potential treatment of prostate and breast cancer.

Kandil S, Westwell AD, McGuigan C.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2000-4. doi: 10.1016/j.bmcl.2016.02.088. Epub 2016 Mar 2.

26.

Synthesis and in vitro anticancer evaluation of some 4,6-diamino-1,3,5-triazine-2-carbohydrazides as Rad6 ubiquitin conjugating enzyme inhibitors.

Kothayer H, Spencer SM, Tripathi K, Westwell AD, Palle K.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2030-4. doi: 10.1016/j.bmcl.2016.02.085. Epub 2016 Mar 2.

27.

Novel cis-selective and non-epimerisable C3 hydroxy azapodophyllotoxins targeting microtubules in cancer cells.

Kandil S, Wymant JM, Kariuki BM, Jones AT, McGuigan C, Westwell AD.

Eur J Med Chem. 2016 Mar 3;110:311-25. doi: 10.1016/j.ejmech.2015.12.037. Epub 2015 Dec 23.

28.

Novel indole-based melatonin analogues substituted with triazole, thiadiazole and carbothioamides: studies on their antioxidant, chemopreventive and cytotoxic activities.

Shirinzadeh H, Ince E, Westwell AD, Gurer-Orhan H, Suzen S.

J Enzyme Inhib Med Chem. 2016 Dec;31(6):1312-21. doi: 10.3109/14756366.2015.1132209. Epub 2016 Jan 8.

PMID:
26745200
29.

Gold nanoparticle conjugated Rad6 inhibitor induces cell death in triple negative breast cancer cells by inducing mitochondrial dysfunction and PARP-1 hyperactivation: Synthesis and characterization.

Haynes B, Zhang Y, Liu F, Li J, Petit S, Kothayer H, Bao X, Westwell AD, Mao G, Shekhar MPV.

Nanomedicine. 2016 Apr;12(3):745-757. doi: 10.1016/j.nano.2015.10.010. Epub 2015 Nov 10. Erratum in: Nanomedicine. 2019 Jun;18:426.

30.

Advances in small-molecule drug discovery for triple-negative breast cancer.

Fosu-Mensah N, Peris MS, Weeks HP, Cai J, Westwell AD.

Future Med Chem. 2015;7(15):2019-39. doi: 10.4155/fmc.15.129. Epub 2015 Oct 23. Review.

PMID:
26495746
31.

Disulfiram-induced cytotoxicity and endo-lysosomal sequestration of zinc in breast cancer cells.

Wiggins HL, Wymant JM, Solfa F, Hiscox SE, Taylor KM, Westwell AD, Jones AT.

Biochem Pharmacol. 2015 Feb 1;93(3):332-42. doi: 10.1016/j.bcp.2014.12.014. Epub 2014 Dec 31.

32.

A novel radiochemical approach to 1-(2'-deoxy-2'-[(18) F]fluoro-β-d-arabinofuranosyl)cytosine ((18) F-FAC).

Meyer JP, Probst KC, Trist IM, McGuigan C, Westwell AD.

J Labelled Comp Radiopharm. 2014 Sep;57(11):637-44. doi: 10.1002/jlcr.3233. Epub 2014 Sep 25.

PMID:
25257474
33.

Synthesis, anti-HIV and cytostatic evaluation of 3'-deoxy-3'-fluorothymidine (FLT) pro-nucleotides.

Velanguparackel W, Hamon N, Balzarini J, McGuigan C, Westwell AD.

Bioorg Med Chem Lett. 2014 May 15;24(10):2240-3. doi: 10.1016/j.bmcl.2014.03.092. Epub 2014 Apr 5.

PMID:
24751439
34.

Radiochemical synthesis of 2'-[18F]-labelled and 3'-[18F]-labelled nucleosides for positron emission tomography imaging.

Meyer JP, Probst KC, Westwell AD.

J Labelled Comp Radiopharm. 2014 May 15;57(5):333-7. doi: 10.1002/jlcr.3197. Epub 2014 Apr 1. Review.

PMID:
24692121
35.

Design, synthesis and in vitro anticancer evaluation of 4,6-diamino-1,3,5-triazine-2-carbohydrazides and -carboxamides.

Kothayer H, Elshanawani AA, Abu Kull ME, El-Sabbagh OI, Shekhar MP, Brancale A, Jones AT, Westwell AD.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6886-9. doi: 10.1016/j.bmcl.2013.09.087. Epub 2013 Oct 6.

PMID:
24153206
36.

Oxidative stress in carcinogenesis: new synthetic compounds with dual effects upon free radicals and cancer.

Tekiner-Gulbas B, Westwell AD, Suzen S.

Curr Med Chem. 2013;20(36):4451-9. Review.

PMID:
23834180
37.

Synthesis and antioxidant properties of substituted 2-phenyl-1H-indoles.

Karaaslan C, Kadri H, Coban T, Suzen S, Westwell AD.

Bioorg Med Chem Lett. 2013 May 1;23(9):2671-4. doi: 10.1016/j.bmcl.2013.02.090. Epub 2013 Mar 1.

PMID:
23540647
38.

Synthesis and evaluation of 3-(benzylthio)-5-(1H-indol-3-yl)-1,2,4-triazol-4-amines as Bcl-2 inhibitory anticancer agents.

Hamdy R, Ziedan N, Ali S, El-Sadek M, Lashin E, Brancale A, Jones AT, Westwell AD.

Bioorg Med Chem Lett. 2013 Apr 15;23(8):2391-4. doi: 10.1016/j.bmcl.2013.02.029. Epub 2013 Feb 14.

PMID:
23474389
39.

Novel inhibitors of Rad6 ubiquitin conjugating enzyme: design, synthesis, identification, and functional characterization.

Sanders MA, Brahemi G, Nangia-Makker P, Balan V, Morelli M, Kothayer H, Westwell AD, Shekhar MPV.

Mol Cancer Ther. 2013 Apr;12(4):373-83. doi: 10.1158/1535-7163.MCT-12-0793. Epub 2013 Jan 21.

40.

Medicinal chemistry: the academic perspective.

Westwell AD.

Future Med Chem. 2013 Jan;5(1):21-3. doi: 10.4155/fmc.12.146. No abstract available.

PMID:
23256809
41.

Synthesis and evaluation of indole-containing 3,5-diarylisoxazoles as potential pro-apoptotic antitumour agents.

Md Tohid SF, Ziedan NI, Stefanelli F, Fogli S, Westwell AD.

Eur J Med Chem. 2012 Oct;56:263-70. doi: 10.1016/j.ejmech.2012.08.009. Epub 2012 Aug 14.

PMID:
22955095
42.

The identification and chemical characterization of a new arylcyclohexylamine, methoxetamine, using a novel Emergency Department toxicosurveillance tool.

Westwell AD, Hutchings A, Caldicott DG.

Drug Test Anal. 2013 Mar;5(3):203-7. doi: 10.1002/dta.1375. Epub 2012 Jun 26. No abstract available.

PMID:
22733704
43.

The dark side of pharmaceutical chemistry.

Westwell AD, Caldicott DG, Hutchings A.

Future Med Chem. 2012 Feb;4(2):129-32. doi: 10.4155/fmc.11.186. No abstract available.

PMID:
22300092
44.

Design, synthesis and pro-apoptotic antitumour properties of indole-based 3,5-disubstituted oxadiazoles.

Ziedan NI, Stefanelli F, Fogli S, Westwell AD.

Eur J Med Chem. 2010 Oct;45(10):4523-30. doi: 10.1016/j.ejmech.2010.07.012. Epub 2010 Jul 21.

PMID:
20705365
45.

Homology Modelling of Human E1 Ubiquitin Activating Enzyme.

Brahemi G, Burger AM, Westwell AD, Brancale A.

Lett Drug Des Discov. 2010 Jan 1;7(1):57-62.

46.

Exploring the structural requirements for inhibition of the ubiquitin E3 ligase breast cancer associated protein 2 (BCA2) as a treatment for breast cancer.

Brahemi G, Kona FR, Fiasella A, Buac D, Soukupová J, Brancale A, Burger AM, Westwell AD.

J Med Chem. 2010 Apr 8;53(7):2757-65. doi: 10.1021/jm901757t.

47.

Tuning the pH sensitivities of orthoester based compounds for drug delivery applications by simple chemical modification.

Bruyère H, Westwell AD, Jones AT.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2200-3. doi: 10.1016/j.bmcl.2010.02.035. Epub 2010 Feb 13.

PMID:
20207145
48.

The role and future potential of fluorinated biomarkers in positron emission tomography.

Daniels S, Tohid SF, Velanguparackel W, Westwell AD.

Expert Opin Drug Discov. 2010 Mar;5(3):291-304. doi: 10.1517/17460441003652967.

PMID:
22823024
49.

Cinnamaldehydes inhibit thioredoxin reductase and induce Nrf2: potential candidates for cancer therapy and chemoprevention.

Chew EH, Nagle AA, Zhang Y, Scarmagnani S, Palaniappan P, Bradshaw TD, Holmgren A, Westwell AD.

Free Radic Biol Med. 2010 Jan 1;48(1):98-111. doi: 10.1016/j.freeradbiomed.2009.10.028. Epub 2009 Oct 27.

PMID:
19837157
50.

Structure-activity analysis of 2'-modified cinnamaldehyde analogues as potential anticancer agents.

Gan FF, Chua YS, Scarmagnani S, Palaniappan P, Franks M, Poobalasingam T, Bradshaw TD, Westwell AD, Hagen T.

Biochem Biophys Res Commun. 2009 Oct 2;387(4):741-7. doi: 10.1016/j.bbrc.2009.07.104. Epub 2009 Jul 25.

PMID:
19635456

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