Professor Andrew Westwell

Professor of Medicinal Chemistry

School of Pharmacy and Pharmaceutical Sciences

: WestwellA@cardiff.ac.uk
: +44 29208 75800

: Media commentator

I joined the School of Pharmacy & Pharmaceutical Sciences in January 2006. My research interests:

Anticancer drug discovery,
18F PET radiochemistry
Chemical analysis of new psychoactive substances.

In particular, my research focuses on the discovery and pre-clinical development of new molecules targeting metastatic progression, the cause of death in >90% of cancer patients.

Qualifications

PhD in synthetic organic chemistry, University of Leeds (1990-1993)
BSc (Hons) Chemistry, University of Leeds (1987-1990)

2020

Hamdy, R., Elseginy, S. A., Ziedan, N. I., El-Sadek, M., Lashin, E., Jones, A. T. and Westwell, A. D. 2020. Design, synthesis and evaluation of new bioactive oxadiazole derivatives as anticancer agents targeting Bcl-2. International Journal of Molecular Sciences 21(23), article number: 8980. (10.3390/ijms21238980)
Kandil, S. B., Jones, S. R., Smith, S., Hiscox, S. E. and Westwell, A. D. 2020. Structure-based virtual screening, synthesis and biological evaluation of potential FAK-FAT domain inhibitors for treatment of metastatic cancer. Molecules 25(15), article number: 3488. (10.3390/molecules25153488)
Cavaliere, A. et al. 2020. Radiosynthesis of [18F]-labelled pro-nucleotides (ProTides). Molecules 25(3), article number: 704. (10.3390/molecules25030704)

2019

Kandil, S., Pannecouque, C., Chapman, F. M., Westwell, A. D. and McGuigan, C. 2019. Polyfluoroaromatic stavudine (d4T) ProTides exhibit enhanced anti-HIV activity. Bioorganic and Medicinal Chemistry Letters 29(24), article number: 126721. (10.1016/j.bmcl.2019.126721)
Pertusati, F., Ferla, S., Bassetto, M., Brancale, A., Kandil, S., Westwell, A. D. and McGuigan, C. 2019. A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer. European Journal of Medicinal Chemistry 180, pp. 1-14. (10.1016/j.ejmech.2019.07.001)
Crusco, A. et al. 2019. Antischistosomal properties of sclareol and its heck-coupled derivatives: Design, synthesis, biological evaluation, and untargeted metabolomics. ACS Infectious Diseases 5(7), pp. 1188-1199. (10.1021/acsinfecdis.9b00034)
Crusco, A., Baptista, R., Bhowmick, S., Beckmann, M., Mur, L. A. J., Westwell, A. D. and Hoffmann, K. F. 2019. The anti-mycobacterial activity of a diterpenoid-like molecule operates through nitrogen and amino acid starvation. Frontiers in Microbiology 10, article number: 1444. (10.3389/fmicb.2019.01444)
Hamdy, R., Elseginy, S., Ziedan, N., Jones, A. and Westwell, A. 2019. New quinoline-based heterocycles as anticancer agents targeting Bcl-2. Molecules 24(7), pp. 1274. (10.3390/molecules24071274)
Kandil, S., Lee, K. Y., Davies, L., Rizzo, S. A., Dart, D. A. and Westwell, A. D. 2019. Discovery of deshydroxy bicalutamide derivatives as androgen receptor antagonists. European Journal of Medicinal Chemistry 167, pp. 49-60. (10.1016/j.ejmech.2019.01.054)
Anderson, R. L. et al. 2019. A framework for the development of effective anti-metastatic agents. Nature Reviews Clinical Oncology 16, pp. 185-204. (10.1038/s41571-018-0134-8)
James, E., Robertshaw, T. L. and Westwell, A. D. 2019. Emerging from the dark side: new therapeutic applications of scheduled psychoactive substances. Future Medicinal Chemistry 11(3) (10.4155/fmc-2018-0447)
Fosu-Mensah, N. A., Jiang, W., Brancale, A., Cai, J. and Westwell, A. D. 2019. The discovery of purine-based agents targeting triple-negative breast cancer and the αB-crystallin/VEGF protein-protein interaction. Medicinal Chemistry Research 28(2), pp. 182-202. (10.1007/s00044-018-2275-9)
Kourti, M., Westwell, A., Jiang, W. and Cai, J. 2019. Repurposing old carbon monoxide-releasing molecules towards the anti-angiogenic therapy of triple-negative breast cancer. Oncotarget 10(10), pp. 1132-1148. (10.18632/oncotarget.26638)
James, E., Robertshaw, T., Chapman, F. M., Westwell, A. D. and Smith, A. P. 2019. Using the pharmacy retail model to examine perceptions and biases of a UK population sample towards regulation of specific psychoactive drugs.. Drug Science, Policy and Law 5 (10.1177/2050324519876123)

2018

Shirinzadeh, H., Suzen, S., Altanlar, N. and Westwell, A. 2018. Antimicrobial activities of new indole derivatives containing 1,2,4-Triazole, 1,3,4-Thiadiazole and Carbothioamide. The Turkish Journal of Pharmaceutical Sciences 15(3), pp. 291-297. (10.4274/tjps.55707)
Dart, D. A., Kandil, S., Tommasini-Ghelfi, S., Almeida, G. S. d., Bevan, C. L., Jiang, W. G. and Westwell, A. D. 2018. Novel trifluoromethylated enobosarm analogues with potent antiandrogenic activity in vitro and tissue selectivity in vivo. Molecular Cancer Therapeutics 17(9), pp. 1846-1858. (10.1158/1535-7163.MCT-18-0037)
Crusco, A., Bordoni, C., Chakroborty, A., Whatley, K. C., Whiteland, H., Westwell, A. D. and Hoffmann, K. F. 2018. Design, synthesis and anthelmintic activity of 7-keto-sempervirol analogues. European Journal of Medicinal Chemistry 152, pp. 87-100. (10.1016/j.ejmech.2018.04.032)
James, E., Robertshaw, T., Westwell, A. and Smith, A. 2018. Pharmacies as potential providers of harm reduction services: A preliminary online survey. Drug Science, Policy and Law 4, pp. 1-14. (10.1177/2050324518767441)
Kandil, S., Prencipe, F., Jones, S., Hiscox, S. and Westwell, A. D. 2018. The discovery of new and more potent chloropyramine (C4) analogues for the potential treatment of invasive breast cancer. Chemical Biology and Drug Design 91(1), pp. 314-321. (10.1111/cbdd.13083)

2017

Somasagara, R. R. et al. 2017. RAD6 promotes DNA repair and stem cell signaling in ovarian cancer and is a promising therapeutic target to prevent and treat acquired chemoresistance. Oncogene 36, pp. 6680-6690. (10.1038/onc.2017.279)
Cavaliere, A., Probst, K., Westwell, A. and Slusarczyk, M. 2017. Fluorinated nucleosides as an important class of anticancer and antiviral agents. Future Medicinal Chemistry 9(15)
Hendriks, H. R., Govaerts, A., Fichtner, I., Burtles, S., Westwell, A. and Peters, G. J. 2017. Pharmacologically directed strategies in academic anticancer drug discovery based on the European NCI compounds initiative. British Journal of Cancer 117, pp. 195-202. (10.1038/bjc.2017.167)
Bassetto, M., Ferla, S., Giancotti, G., Pertusati, F., Westwell, A. D., Brancale, A. and McGuigan, C. 2017. Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. MedChemComm 8(7), pp. 1414-1420. (10.1039/C7MD00164A)
Hamdy, R. et al. 2017. Synthesis and evaluation of 5-(1H-indol-3-yl)-N-aryl-1,3,4-oxadiazol-2-amines as Bcl-2 inhibitory anticancer agents. Bioorganic & Medicinal Chemistry Letters 27(4), pp. 1037-1040. (10.1016/j.bmcl.2016.12.061)
Ziedan, N. I. et al. 2017. Virtual screening, SAR and discovery of 5-(indole-3-yl)-2-[(2-nitrophenyl)amino] [1,3,4]-oxadiazole as a novel Bcl-2 inhibitor. Chemical Biology and Drug Design (10.1111/cbdd.12936)

2016

Wymant, J., Hiscox, S., Westwell, A., Urbe, S., Clague, M. and Jones, A. T. 2016. The Role of BCA2 in the endocytic trafficking of EGFR and significance as a prognostic biomarker in cancer. Journal of Cancer 7(15), pp. 2388-2407. (10.7150/jca.15055)
Kandil, S., Balzarini, J., Rat, S., Brancale, A., Westwell, A. D. and McGuigan, C. 2016. ProTides of BVdU as potential anticancer agents upon efficient intracellular delivery of their activated metabolites. Biorganic and Medicinal Chemistry Letters 26(23), pp. 5618-5623. (10.1016/j.bmcl.2016.10.077)
Bassetto, M., Ferla, S., Pertusati, F., Kandil, S., Westwell, A., Brancale, A. and McGuigan, C. 2016. Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. European Journal of Medicinal Chemistry 118, pp. 230-243. (10.1016/j.ejmech.2016.04.052)
Ferla, S., Bassetto, M., Pertusati, F., Kandil, S., Westwell, A. D., Brancale, A. and McGuigan, C. 2016. Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. Bioorganic and Medicinal Chemistry Letters 26(15), pp. 3636-3640. (10.1016/j.bmcl.2016.06.001)
Haynes, B. et al. 2016. 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: Nanotechnology, Biology and Medicine 12(3), pp. 745-757. (10.1016/j.nano.2015.10.010)
Kothayer, H., Spencer, S. M., Tripathi, K., Westwell, A. D. and Palle, K. 2016. Synthesis and in vitro anticancer evaluation of some 4,6-diamino-1,3,5-triazine-2-carbohydrazides as Rad6 ubiquitin conjugating enzyme inhibitors. Biorganic and Medicinal Chemistry Letters 26(8), pp. 2030-2034. (10.1016/j.bmcl.2016.02.085)
Kandil, S., Wymant, J., Kariuki, B., Jones, A. T., McGuigan, C. and Westwell, A. D. 2016. Novel cis-selective and non-epimerisable C3 hydroxy azapodophyllotoxins targeting microtubules in cancer cells. European Journal of Medicinal Chemistry 110, pp. 311-325. (10.1016/j.ejmech.2015.12.037)
Shirinzadeh, H., Ince, E., Westwell, A. D., Gurer-Orhan, H. and Suzen, S. 2016. Novel indole-based melatonin analogues substituted with triazole, thiadiazole and carbothioamides: studies on their antioxidant, chemopreventive and cytotoxic activities. Journal of Enzyme Inhibition and Medicinal Chemistry 31(6), pp. 1312-1321. (10.3109/14756366.2015.1132209)
Kandil, S., Westwell, A. D. and McGuigan, C. 2016. 7-Substituted umbelliferone derivatives as androgen receptor antagonists for the potential treatment of prostate and breast cancer. Biorganic and Medicinal Chemistry Letters 26(8), pp. 2000-2004. (10.1016/j.bmcl.2016.02.088)
Westwell, A. D. ed. 2016. Fluorinated pharmaceuticals: advances in medicinal chemistry. Future Medicine. (10.4155/9781909453968)

2015

Edwards, R., de Vries, W., Westwell, A. D., Daniels, S. and Wirth, T. 2015. Solid-supported iodonium salts for fluorinations. European Journal of Organic Chemistry 2015(31), pp. 6909-6916. (10.1002/ejoc.201500992)
Cilibrasi, V., Tsang, K. Y. I., Morelli, M., Solfa, F., Wiggins, H., Jones, A. T. and Westwell, A. D. 2015. Synthesis of substituted carbamo(dithioperoxo)thioates as potential BCA2-inhibitory anticancer agents. Tetrahedron Letters 56(20), pp. 2583-2585. (10.1016/j.tetlet.2015.03.132)
Wiggins, H. L., Wymant, J. M., Solfa, F., Hiscox, S. E., Taylor, K. M., Westwell, A. D. and Jones, A. T. 2015. Disulfiram-induced cytotoxicity and endo-lysosomal sequestration of zinc in breast cancer cells. Biochemical Pharmacology 93(3), pp. 332-342. (10.1016/j.bcp.2014.12.014)
Edwards, R., Westwell, A. D., Daniels, S. and Wirth, T. 2015. Convenient synthesis of diaryliodonium salts for the production of [18F]F-DOPA. European Journal of Organic Chemistry 2015(3), pp. 625-630. (10.1002/ejoc.201403378)
Fosu-Mensah, N., Peris, M. S., Weeks, H. P., Cai, J. and Westwell, A. D. 2015. Advances in small-molecule drug discovery for triple-negative breast cancer. Future Medicinal Chemistry 7(15), pp. 2019-2039. (10.4155/fmc.15.129)

2014

Meyer, J., Probst, K. C., Trist, I. M., McGuigan, C. and Westwell, A. D. 2014. A novel radiochemical approach to 1-(2 '-deoxy-2 '-[F-18] fluoro-beta-D-arabinofuranosyl)cytosine (F-18-FAC). Journal of Labelled Compounds and Radiopharmaceuticals 57(11), pp. 637-644. (10.1002/jlcr.3233)
Meyer, J., Probst, K. C. and Westwell, A. D. 2014. Radiochemical synthesis of 2′-[18F]-labelled and 3′-[18F]-labelled nucleosides for positron emission tomography imaging. Journal of Labelled Compounds and Radiopharmaceuticals 57(5), pp. 333-337. (10.1002/jlcr.3197)
Velanguparackel, W., Hamon, N., Balzarini, J., McGuigan, C. and Westwell, A. D. 2014. Synthesis, anti-HIV and cytostatic evaluation of 3′-deoxy-3′-fluorothymidine (FLT) pro-nucleotides. Bioorganic and Medicinal Chemistry Letters 24(10), pp. 2240-2243. (10.1016/j.bmcl.2014.03.092)

2013

Kothayer, H. et al. 2013. Design, synthesis and in vitro anticancer evaluation of 4,6-diamino-1,3,5-triazine-2-carbohydrazides and -carboxamides. Biorganic and Medicinal Chemistry Letters 23(24), pp. 6886-6889. (10.1016/j.bmcl.2013.09.087)
Hamdy, R. et al. 2013. Synthesis and evaluation of 3-(benzylthio)-5-(1H-indol-3-yl)-1,2,4-triazol-4-amines as Bcl-2 inhibitory anticancer agents. Biorganic and Medicinal Chemistry Letters 23(8), pp. 2391-2394. (10.1016/j.bmcl.2013.02.029)
Sanders, M. A. et al. 2013. Novel inhibitors of Rad6 ubiquitin conjugating enzyme: Design, synthesis, identification, and functional characterization. Molecular Cancer Therapeutics 12(4), pp. 373-383. (10.1158/1535-7163.MCT-12-0793)
Tekiner-Gulbas, B., Westwell, A. D. and Suzen, S. 2013. Oxidative stress in carcinogenesis: new synthetic compounds with dual effects upon free radicals and cancer. Current Medicinal Chemistry 20(36), pp. 4451-4459. (10.2174/09298673113203690142)
Weekes, A. A., Frydrych, J. and Westwell, A. D. 2013. Convenient synthesis of substituted 2-phenylbenzothiazoles using solid-supported triphenylphosphine. Synthetic Communications 43(19), pp. 2656-2662. (10.1080/00397911.2012.730648)
Karaaslan, C., Kadri, H., Coban, T., Suzen, S. and Westwell, A. D. 2013. Synthesis and antioxidant properties of substituted 2-phenyl-1H-indoles. Biorganic and Medicinal Chemistry Letters 23(9), pp. 2671-2674. (10.1016/j.bmcl.2013.02.090)
Westwell, A. D., Hutchings, A. and Caldicott, D. G. E. 2013. The identification and chemical characterization of a new arylcyclohexylamine, methoxetamine, using a novel Emergency Department toxicosurveillance tool. Drug Testing and Analysis 5(3), pp. 203-207. (10.1002/dta.1375)

2012

Soukupova, J., Brancale, A., Westwell, A. D. and Clarkson, R. W. E. 2012. Inhibitors of Bcl-3 as a novel therapeutic strategy for HER2+ breast cancer. European Journal of Cancer 48(5), pp. S225-S225.
Md Tohid, S. F., Ziedan, N. I., Stefanelli, F., Fogli, S. and Westwell, A. D. 2012. Synthesis and evaluation of indole-containing 3,5-diarylisoxazoles as potential pro-apoptotic antitumour agents. European Journal of Medicinal Chemistry 56, pp. 263-270. (10.1016/j.ejmech.2012.08.009)

2011

Cottens, S. et al. 2011. Ask the experts: future of the pharmaceutical industry. Future Medicinal Chemistry 3(15) (10.4155/fmc.11.145)
Altug, C. et al. 2011. An efficient one-pot multicomponent approach to 5-amino-7-aryl-8-nitrothiazolo[3,2-a]pyridines. Tetrahedron 67(49), pp. 9522-9528. (10.1016/j.tet.2011.10.005)
Weekes, A. A., Bagley, M. C. and Westwell, A. D. 2011. An efficient synthetic route to biologically relevant 2-phenylbenzothiazoles substituted on the benzothiazole ring. Tetrahedron 67(40), pp. 7743-7747. (10.1016/j.tet.2011.08.004)

2010

Ziedan, N. I., Stefanelli, F., Fogli, S. and Westwell, A. D. 2010. Design, synthesis and pro-apoptotic antitumour properties of indole-based 3,5-disubstituted oxadiazoles. European Journal of Medicinal Chemistry 45(10), pp. 4523-4530. (10.1016/j.ejmech.2010.07.012)
Brahemi, G. et al. 2010. Exploring the structural requirements for inhibition of the ubiquitin E3 ligase breast cancer associated protein 2 (BCA2) as a treatment for breast cancer. Journal of Medicinal Chemistry 53(7), pp. 2757-2765. (10.1021/jm901757t)
Chew, E. et al. 2010. Cinnamaldehydes inhibit thioredoxin reductase and induce Nrf2: potential candidates for cancer therapy and chemoprevention. Free Radical Biology & Medicine 48(1), pp. 98-111. (10.1016/j.freeradbiomed.2009.10.028)
Brahemi, G., Burger, A. M., Westwell, A. and Brancale, A. 2010. Homology Modelling of Human E1 Ubiquitin Activating Enzyme. Letters in Drug Design & Discovery 7(1), pp. 57-62. (10.2174/157018010789869316)
Bruyere, H., Westwell, A. and Jones, A. T. 2010. Tuning the pH sensitivities of orthoester based compounds for drug delivery applications by simple chemical modification. Bioorganic & Medicinal Chemistry Letters 20(7), pp. 2200-2203. (10.1016/j.bmcl.2010.02.035)
Daniels, S., Md Tohid, S. F., Velanguparackel, W. and Westwell, A. 2010. The role and future potential of fluorinated biomarkers in positron emission tomography. Expert Opinion on Drug Discovery 5(3), pp. 291-304. (10.1517/17460441003652967)
Weekes, A. A., Dix, M. C., Bagley, M. C. and Westwell, A. D. 2010. Rapid and convenient thermal or microwave-assisted synthesis of substituted 2-Phenylbenzothiazoles. Synthetic Communications 40(20), pp. 3027-3032. (10.1080/00397910903353739)

2009

Gan, F. F. et al. 2009. Structure-activity analysis of 2 '-modified cinnamaldehyde analogues as potential anticancer agents. Biochemical and Biophysical Research Communications 387(4), pp. 741-747. (10.1016/j.bbrc.2009.07.104)
Weekes, A. A. and Westwell, A. 2009. 2-Arylbenzothiazole as a Privileged Scaffold in Drug Discovery. Current Medicinal Chemistry 16(19), pp. 2430-2440.

2008

Kadri, H., Dale, T. C., Ewan, K. B. R. and Westwell, A. 2008. The design, synthesis and antitumour evaluation of novel small molecule inhibitors of the Dishevelled PDZ domain [Poster Presentation/Abstract]. EJC Supplements 6(12), pp. 137., article number: 436. (10.1016/S1359-6349(08)72370-X)
Huber, K. et al. 2008. 2- [(1-methylpropyl)dithio] -1H-imidazole inhibits tubulin polymerization through cysteine oxidation. Molecular Cancer Therapeutics 7(1), pp. 143-151. (10.1158/1535-7163.mct-07-0486)
Aiello, S. et al. 2008. 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). Journal of Medicinal Chemistry 51(16), pp. 5135-5139. (10.1021/jm800418z)
Brahemi, G., Fiasella, A., Brancale, A., Westwell, A. and Burger, A. 2008. Design and synthesis of BCA2 inhibitors. EJC Supplements 6(12), pp. 44.
Callister, M. et al. 2008. PMX464, a thiol-reactive quinol and putative thioredoxin inhibitor, inhibits NF-kappa B-dependent proinflammatory activation of alveolar epithelial cells. British Journal of Pharmacology 155(5), pp. 661-672. (10.1038/bjp.2008.258)
Kadri, H., Matthews, C. S., Bradshaw, T. D., Stevens, M. F. G. and Westwell, A. 2008. Synthesis and antitumour evaluation of novel 2-phenylbenzimidazoles. Journal of Enzyme Inhibition and Medicinal Chemistry 23(5), pp. 641-647. (10.1080/14756360802205398)
Westwell, A. 2008. Advances in Cancer Drug Discovery - A British Association for Cancer Research Meeting. IDrugs 11(11), pp. 783-786.
White, A. W., Westwell, A. and Brahemi, G. 2008. Protein-protein interactions as targets for small-molecule therapeutics in cancer. Expert Reviews in Molecular Medicine 10(e8), pp. 1-14. (10.1017/S1462399408000641)
Ziedan, N., Kadri, H. and Westwell, A. 2008. The development of pro-apoptotic cancer therapeutics. Mini-Reviews in Medicinal Chemistry 8(7), pp. 711-718.
Ziedan, N., Westwell, A. and Fogli, S. 2008. Design and synthesis of novel indole derivatives as selective apoptosis-inducers. EJC Supplements 6(12), pp. 45-46.

2007

Athanasiou, A. et al. 2007. Cannabinoid receptor agonists are mitochondrial inhibitors: A unified hypothesis of how cannabinoids modulate mitochondrial function and induce cell death. Biochemical and Biophysical Research Communications 364(1), pp. 131-137. (10.1016/j.bbrc.2007.09.107)
Athanasiou, A. et al. 2007. Vanilloid receptor agonists and antagonists are mitochondrial inhibitors: how vanilloids cause non-vanilloid receptor mediated cell death. Biochemical and Biophysical Research Communications 354(1), pp. 50-55. (10.1016/j.bbrc.2006.12.179)
Henriksen, G., Hauser, A. I., Westwell, A., Yousefi, B. H., Schwaiger, M., Drzezga, A. and Wester, H. J. 2007. Metabolically stabilized benzothiazoles for imaging of amyloid plaques. Journal of Medicinal Chemistry 50(6), pp. 1087-1089. (10.1021/jm061466g)
Matsuura, T., Harrison, R. A., Westwell, A., Nakamura, H., Martynyuk, A. E. and Sumners, C. 2007. Basal and angiotensin II-inhibited neuronal delayed-rectifier K+ current are regulated by thioredoxin. American Journal of Physiology -Cell Physiology 293(1), pp. C211-C217. (10.1152/ajpcell.00615.2006)
Shah, P. and Westwell, A. 2007. The role of fluorine in medicinal chemistry. Journal of Enzyme Inhibition and Medicinal Chemistry 22(5), pp. 527-540. (10.1080/14756360701425014)

2006

Westwell, A. D., Mortimer, C., Wells, G. and Crochard, J. 2006. Antitumor benzothiazoles. 26. 2-(3,4-Dimethoxyphenyl)-5-fluorobenzothiazole (GW 610, NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and selective inhibitory activity against lung, colon, and breast cancer cell lines. Journal of Medicinal Chemistry 49(1), pp. 179-185. (10.1021/jm050942k)

2005

Westwell, A. D., Berry, J., Bradshaw, T. and Fichtner, I. 2005. Quinols as novel therapeutic agents. 2. 4-(1-Arylsulfonylindol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-ones and related agents as potent and selective antitumor agents. Journal of Medicinal Chemistry 48(2), pp. 639-644. (10.1021/jm040859h)

2003

Westwell, A. D., Wells, G., Berry, J. and Bradshaw, T. 2003. 4-Substituted-4-hydroxycyclohexa-2,5-dien-1-ones with selective activities against colon and renal cancer cell lines. Journal of Medicinal Chemistry 46(4), pp. 532-541. (10.1021/jm020984y)

2001

Hutchinson, I., Chua, M., Browne, H. L., Trapani, V., Bradshaw, T. D., Westwell, A. D. and Stevens, M. F. G. 2001. Antitumor benzothiazoles. 14. Synthesis and in vitro biological properties of fluorinated 2-(4-aminophenyl)benzothiazoles. Journal of Medicinal Chemistry 44(9), pp. 1446-1455. (10.1021/jm001104n)

Research interests

Having trained in synthetic organic chemistry, the main focus of my research activities in recent years has been in the area of medicinal chemistry and cancer drug discovery.

I am a medicinal chemist with extensive experience of the design, synthesis and biological evaluation of small molecules for drug discovery and diagnostics. My research interests can be divided into the following categories:

Anti-metastatic drug discovery (Bcl-3 inhibition)
Targeting cancer stem cells for selective apoptosis (c-Flip inhibition)
New theranostic pro-nucleotides (ProTides)
New androgen receptor antagonists (prostate cancer)
New FAK inhibitors (invasive breast cancer)
Natural product derivatives targeting schistosomiasis
Diagnostic imaging (Positron Emission Tomography) via ¹⁸F radiochemistry
Characterisation of novel psychoactive substances, from a harm reduction perspective

Cancer drug design and discovery

Previously I have been involved in a variety of cancer drug discovery projects, using cell-based screening methods to identify new compounds of interest. One of these discovery projects has resulted in the identification of a new agent in clinical trial (Phortress). Current research interests are directed towards the following areas:

a breast cancer associated E3 ubiquitin ligase (BCA2) and E2 ubiquitin-conjugating enzyme (Rad6B)
protein-protein interaction targets in cancer
selective induction of apoptosis in cancer cells
Diagnostic imaging in cancer and neuroscience using Positron Emission Tomography. Interests in this area centre on the discovery of new F-labelled aromatic molecules for potential diagnostic PET imaging applications, and chemical methodologies for the late stage installation of fluoride into aromatic therapeutic and diagnostic agents.
Characterisation of novel psychoactive substances (WEDINOS Project)
Use of analytical chemical methods (NMR and LCMS) to characterise new psychoactives, including 'legal highs'. This work is carried out in conjunction with Public Health Wales and Llandough Hospital Cardiff

Collaborators

Cardiff University

Prof. Andrea Brancale (School of Pharmacy and Pharmaceutical Sciences)
Prof. Richard Clarkson (School of Biosciences)
Prof. Arwyn Jones (School of Pharmacy and Pharmaceutical Sciences)
Dr. Stephen Hiscox (School of Pharmacy and Pharmaceutical Sciences)

External

Josie Smith, Dean Acreman, Joanne Rogers, Mary Busby (WEDINOS project, Public Health Wales and NHS Wales)
Prof. Karl Hoffmann (Aberystwyth University, Wales)

Key Expertise

Medicinal chemistry and drug design
Analytical spectroscopy (NMR, mass spectrometry)

Current research funding

2020-21 Wellcome Trust / Cardiff University ISSF3 Translational Kickstart: Development of Novel Theranostic Pro-Nucleotides (ProTides). PI: Andrew Westwell.
2012- Public Health Wales (Welsh Government) / NHS Wales: New Psychoactive Substances Project – Action in Wales. PI: Josie Smith. Contribution: drug analysis by NMR spectroscopy.

PH1125 Chemical and biological properties of drug molecules
PH2112 Principles of drug design
PH3101 Optimisation of drug design
PH3202 Research methodology
PH4116 Pharmacy research or scholarship project
PH4117 Pharmaceutical sciences, pharmacy practice and the population

Career profile

I graduated with a degree in Chemistry from the University of Leeds in 1990, and then completed a PhD in synthetic organic chemistry from the same department under the supervision of Professor Chris Rayner. Following a two-year postdoctoral position in the Department of Chemistry at Loughborough University under the supervision of Professor Jonathan Williams then Professor Chris Moody, I was appointed as a Research Fellow within the Cancer Research Laboratories at the University of Nottingham, with Professor Malcolm Stevens. I was appointed to a Cancer Research UK funded Lectureship in 2001 in the School of Pharmacy at Nottingham, and moved to the School of Pharmacy and Pharmaceutical Science in 2006 to take up a position as Senior Lecturer in Medicinal Chemistry. I was promoted to Reader in 2013.

Scientific and professional service

I am recent past-Treasurer for the British Association for Cancer Research, a charitable organisation of over 1000 cancer professionals, and have been involved in the organisation of a number of cancer research-related conferences.

Prizes / membership of professional bodies

Royal Society of Chemistry Malcolm Campbell memorial prize winner 2003 (with MFG Stevens and TD Bradshaw)

Cardiff University to offer coronavirus tests to thousands of staff and students