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Items: 1 to 50 of 84

1.

Novel Trifluoromethylated Enobosarm Analogues with Potent Anti-androgenic 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 Jun 12. pii: molcanther.0037.2018. doi: 10.1158/1535-7163.MCT-18-0037. [Epub ahead of print]

PMID:
29895558
2.

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.

3.

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
4.

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
5.

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.

6.

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.

PMID:
28609434
7.

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
8.

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
9.

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.

10.

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.

11.

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
12.

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.

13.

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.

14.

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.

15.

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.

16.

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
17.

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.

18.

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
19.

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.

20.

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
21.

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
22.

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
23.

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
24.

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
25.

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
26.

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
27.

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.

28.

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
29.

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
30.

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
31.

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
32.

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
33.

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.

34.

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.

35.

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
36.

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
37.

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
38.

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
39.

2-Arylbenzothiazole as a privileged scaffold in drug discovery.

Weekes AA, Westwell AD.

Curr Med Chem. 2009;16(19):2430-40. Review.

PMID:
19601790
40.
41.

Synthesis and antitumour evaluation of novel 2-phenylbenzimidazoles.

Kadri H, Matthews CS, Bradshaw TD, Stevens MF, Westwell AD.

J Enzyme Inhib Med Chem. 2008 Oct;23(5):641-7. doi: 10.1080/14756360802205398 .

PMID:
18821253
42.

Synthesis and biological properties of benzothiazole, benzoxazole, and chromen-4-one analogues of the potent antitumor agent 2-(3,4-dimethoxyphenyl)-5-fluorobenzothiazole (PMX 610, NSC 721648).

Aiello S, Wells G, Stone EL, Kadri H, Bazzi R, Bell DR, Stevens MF, Matthews CS, Bradshaw TD, Westwell AD.

J Med Chem. 2008 Aug 28;51(16):5135-9. doi: 10.1021/jm800418z. Epub 2008 Jul 31.

PMID:
18666770
43.

PMX464, a thiol-reactive quinol and putative thioredoxin inhibitor, inhibits NF-kappaB-dependent proinflammatory activation of alveolar epithelial cells.

Callister ME, Pinhu L, Catley MC, Westwell AD, Newton R, Leaver SK, Quinlan GJ, Evans TW, Griffiths MJ, Burke-Gaffney A.

Br J Pharmacol. 2008 Nov;155(5):661-72. doi: 10.1038/bjp.2008.258. Epub 2008 Jun 30.

44.

The development of pro-apoptotic cancer therapeutics.

Ziedan NI, Kadri H, Westwell AD.

Mini Rev Med Chem. 2008 Jun;8(7):711-8. Review.

PMID:
18537726
45.

Protein-protein interactions as targets for small-molecule therapeutics in cancer.

White AW, Westwell AD, Brahemi G.

Expert Rev Mol Med. 2008 Mar 19;10:e8. doi: 10.1017/S1462399408000641. Review.

PMID:
18353193
46.

2-[(1-methylpropyl)dithio]-1H-imidazole inhibits tubulin polymerization through cysteine oxidation.

Huber K, Patel P, Zhang L, Evans H, Westwell AD, Fischer PM, Chan S, Martin S.

Mol Cancer Ther. 2008 Jan;7(1):143-51. doi: 10.1158/1535-7163.MCT-07-0486.

47.

The role of fluorine in medicinal chemistry.

Shah P, Westwell AD.

J Enzyme Inhib Med Chem. 2007 Oct;22(5):527-40. Review.

PMID:
18035820
48.

Cannabinoid receptor agonists are mitochondrial inhibitors: a unified hypothesis of how cannabinoids modulate mitochondrial function and induce cell death.

Athanasiou A, Clarke AB, Turner AE, Kumaran NM, Vakilpour S, Smith PA, Bagiokou D, Bradshaw TD, Westwell AD, Fang L, Lobo DN, Constantinescu CS, Calabrese V, Loesch A, Alexander SP, Clothier RH, Kendall DA, Bates TE.

Biochem Biophys Res Commun. 2007 Dec 7;364(1):131-7. Epub 2007 Oct 2.

PMID:
17931597
49.

Basal and angiotensin II-inhibited neuronal delayed-rectifier K+ current are regulated by thioredoxin.

Matsuura T, Harrison RA, Westwell AD, Nakamura H, Martynyuk AE, Sumners C.

Am J Physiol Cell Physiol. 2007 Jul;293(1):C211-7. Epub 2007 Mar 14.

50.

Quinols as novel therapeutic agents. 7.1 Synthesis of antitumor 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxycyclohexa-2,5-dien-1-ones by Sonogashira reactions.

McCarroll AJ, Bradshaw TD, Westwell AD, Matthews CS, Stevens MF.

J Med Chem. 2007 Apr 5;50(7):1707-10. Epub 2007 Mar 8.

PMID:
17343370

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