Professor Andrew Westwell
(he/him)
PhD PGCE HE
- Media commentator
Teams and roles for Andrew Westwell
Professor
Professor of Medicinal Chemistry
Overview
I joined the School of Pharmacy & Pharmaceutical Sciences in January 2006. My research interests:
- Anticancer drug design and discovery (preclinical).
- Chemical analysis of new psychoactive substances.
In particular, my research focuses on the discovery and pre-clinical development of new anticancer drug candidates targeting advanced and metastatic disease, 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)
News
- Innovation and Healthcare Awards - 1 June 2016
- New anti cancer stem cell compound in development - 7 May 2015
Publication
2026
- Kandil, S. B. et al. 2026. Coumarin-stavudine (d4T) novel hybrid ProTides with dual-functionality and enhanced anti-HIV activity. European Journal of Medicinal Chemistry 304 118543. (10.1016/j.ejmech.2025.118543)
2025
- Almehdi, A. M. et al., 2025. Next-generation Bcl-2 inhibitors: design and evaluation of indolyl-triazole derivatives with anticancer potential. ChemMedChem 20 e202500265. (10.1002/cmdc.202500265)
- Bordoni, C. et al. 2025. New anticancer 4‐aryldihydropyrimidinone‐5‐carboxylates targeting Hsp90. Chemical Biology & Drug Design 106 (6) e70221. (10.1111/cbdd.70221)
- Giancotti, G. et al. 2025. The discovery of small-molecule inhibitors of cFLIP that sensitise tumour cells to TNF-related apoptosis-inducing ligand. Academia Oncology 2 (2)(10.20935/AcadOnco7680)
2024
- Scott, A. T. and Westwell, A. D. 2024. Strategies to enhance the racial and ethnic diversity of breast cancer clinical drug trials. Academia Oncology 1 2. (10.20935/acadonco7480)
- Seaton, G. et al. 2024. Multifaceted roles for BCL3 in cancer: a proto-oncogene comes of age. Molecular Cancer 23 (1) 7. (10.1186/s12943-023-01922-8)
2023
- Almehdi, A. M. et al., 2023. Design, synthesis, and potent anticancer activity of novel indole-based Bcl-2 inhibitors. International Journal of Molecular Sciences 24 (19) 14656. (10.3390/ijms241914656)
2022
- Edwards, D. et al. 2022. A rapid scoping review of harm reduction strategies for ecstasy (MDMA) users in recreational settings. [Online].Research Square: Research Square. (10.21203/rs.3.rs-2178425/v1)Available at: https://doi.org/10.21203/rs.3.rs-2178425/v1.
- Scurr, M. et al. 2022. Whole blood-based measurement of SARS-CoV-2-specific T cells reveals asymptomatic infection and vaccine immunogenicity in healthy subjects and patients with solid organ cancers. Immunology 165 (2), pp.250-259. (10.1111/imm.13433)
2021
- Hamdy, R. et al., 2021. New bioactive fused triazolothiadiazoles as Bcl-2-targeted anticancer agents. International Journal of Molecular Sciences 22 (22) 12272. (10.3390/ijms222212272)
- James, E. et al. 2021. Online survey into the development of a model legal framework for a cannabis market in the United Kingdom. Drug Science, Policy and Law 7 (10.1177/20503245211034931)
- Kandil, S. B. et al. 2021. Synthesis, biological evaluation and X-ray analysis of bicalutamide sulfoxide analogues for the potential treatment of prostate cancer. Bioorganic and Medicinal Chemistry Letters 36 127817. (10.1016/j.bmcl.2021.127817)
- Kandil, S. B. , McGuigan, C. and Westwell, A. D. 2021. Synthesis and biological evaluation of bicalutamide analogues for the potential treatment of prostate cancer. Molecules 26 (1) 56. (10.3390/molecules26010056)
- Kourti, M. et al. 2021. Structural modifications on CORM-3 lead to enhanced anti-angiogenic properties against triple-negative breast cancer cells. Medicinal Chemistry 17 (1), pp.40-59. (10.2174/1573406415666191206102452)
- Soukupova, J. et al., 2021. The discovery of a novel anti-metastatic Bcl3 inhibitor. Molecular Cancer Therapeutics 10 (5), pp.775-786. (10.1158/1535-7163.MCT-20-0283)
2020
- Cavaliere, A. et al. 2020. Radiosynthesis of [18F]-labelled pro-nucleotides (ProTides). Molecules 25 (3) 704. (10.3390/molecules25030704)
- Hamdy, R. et al., 2020. Design, synthesis and evaluation of new bioactive oxadiazole derivatives as anticancer agents targeting Bcl-2. International Journal of Molecular Sciences 21 (23) 8980. (10.3390/ijms21238980)
- Kandil, S. B. et al. 2020. Structure-based virtual screening, synthesis and biological evaluation of potential FAK-FAT domain inhibitors for treatment of metastatic cancer. Molecules 25 (15) 3488. (10.3390/molecules25153488)
2019
- 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)
- Crusco, A. et al. 2019. The anti-mycobacterial activity of a diterpenoid-like molecule operates through nitrogen and amino acid starvation. Frontiers in Microbiology 10 1444. (10.3389/fmicb.2019.01444)
- 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)
- Fosu-Mensah, N. A. et al. 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)
- Hamdy, R. et al., 2019. New quinoline-based heterocycles as anticancer agents targeting Bcl-2. Molecules 24 (7), pp.1274. (10.3390/molecules24071274)
- James, E. et al. 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)
- 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)
- Kandil, S. et al. 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)
- Kandil, S. et al. 2019. Polyfluoroaromatic stavudine (d4T) ProTides exhibit enhanced anti-HIV activity. Bioorganic and Medicinal Chemistry Letters 29 (24) 126721. (10.1016/j.bmcl.2019.126721)
- Kourti, M. et al. 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)
- Pertusati, F. et al. 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)
2018
- Crusco, A. et al. 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)
- Dart, D. A. et al. 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)
- James, E. et al. 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. et al. 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)
- Shirinzadeh, H. et al., 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)
2017
- Bassetto, M. et al. 2017. Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. MedChemComm 8 (7), pp.1414-1420. (10.1039/C7MD00164A)
- Cavaliere, A. et al. 2017. Fluorinated nucleosides as an important class of anticancer and antiviral agents. Future Medicinal Chemistry 9 (15)
- 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)
- Hendriks, H. R. et al., 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)
- 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)
- 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
- Bassetto, M. et al. 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. et al. 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)
- Kandil, S. et al. 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)
- 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)
- Kandil, S. et al. 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)
- Kothayer, H. et al., 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)
- Shirinzadeh, H. et al., 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)
- Wymant, J. et al. 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)
2015
- Cilibrasi, V. et al. 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)
- Edwards, R. et al. 2015. Solid-supported iodonium salts for fluorinations. European Journal of Organic Chemistry 2015 (31), pp.6909-6916. (10.1002/ejoc.201500992)
- Edwards, R. et al. 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. et al. 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)
- Wiggins, H. L. et al. 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)
2014
- Meyer, J. et al. 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. et al. 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
- 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)
- Karaaslan, C. et al. 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)
- 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)
- 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)
- 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
- Md Tohid, S. F. et al. 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)
- Soukupova, J. et al., 2012. Inhibitors of Bcl-3 as a novel therapeutic strategy for HER2+ breast cancer. European Journal of Cancer 48 (5), pp.S225-S225.
2011
- 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)
- Cottens, S. et al., 2011. Ask the experts: future of the pharmaceutical industry. Future Medicinal Chemistry 3 (15)(10.4155/fmc.11.145)
- 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
- Brahemi, G. et al. 2010. Homology Modelling of Human E1 Ubiquitin Activating Enzyme. Letters in Drug Design & Discovery 7 (1), pp.57-62. (10.2174/157018010789869316)
- 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)
- 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)
- 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)
- Daniels, S. et al. 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. et al., 2010. Rapid and convenient thermal or microwave-assisted synthesis of substituted 2-Phenylbenzothiazoles. Synthetic Communications 40 (20), pp.3027-3032. (10.1080/00397910903353739)
- Ziedan, N. I. et al., 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)
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
- 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. et al. 2008. Design and synthesis of BCA2 inhibitors. EJC Supplements 6 (12), pp.44.
- 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)
- Kadri, H. et al. 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. 436. (10.1016/S1359-6349(08)72370-X)
- Kadri, H. et al. 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. , 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. et al., 2007. Metabolically stabilized benzothiazoles for imaging of amyloid plaques. Journal of Medicinal Chemistry 50 (6), pp.1087-1089. (10.1021/jm061466g)
- Matsuura, T. et al., 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)
2006
- Westwell, A. D. et al. 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. et al. 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. et al. 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. et al., 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)
Articles
- 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)
- Almehdi, A. M. et al., 2025. Next-generation Bcl-2 inhibitors: design and evaluation of indolyl-triazole derivatives with anticancer potential. ChemMedChem 20 e202500265. (10.1002/cmdc.202500265)
- Almehdi, A. M. et al., 2023. Design, synthesis, and potent anticancer activity of novel indole-based Bcl-2 inhibitors. International Journal of Molecular Sciences 24 (19) 14656. (10.3390/ijms241914656)
- 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)
- 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)
- 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)
- Bassetto, M. et al. 2017. Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. MedChemComm 8 (7), pp.1414-1420. (10.1039/C7MD00164A)
- Bassetto, M. et al. 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)
- Bordoni, C. et al. 2025. New anticancer 4‐aryldihydropyrimidinone‐5‐carboxylates targeting Hsp90. Chemical Biology & Drug Design 106 (6) e70221. (10.1111/cbdd.70221)
- Brahemi, G. et al. 2010. Homology Modelling of Human E1 Ubiquitin Activating Enzyme. Letters in Drug Design & Discovery 7 (1), pp.57-62. (10.2174/157018010789869316)
- Brahemi, G. et al. 2008. Design and synthesis of BCA2 inhibitors. EJC Supplements 6 (12), pp.44.
- 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)
- 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)
- Cavaliere, A. et al. 2017. Fluorinated nucleosides as an important class of anticancer and antiviral agents. Future Medicinal Chemistry 9 (15)
- Cavaliere, A. et al. 2020. Radiosynthesis of [18F]-labelled pro-nucleotides (ProTides). Molecules 25 (3) 704. (10.3390/molecules25030704)
- 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)
- Cilibrasi, V. et al. 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)
- Cottens, S. et al., 2011. Ask the experts: future of the pharmaceutical industry. Future Medicinal Chemistry 3 (15)(10.4155/fmc.11.145)
- Crusco, A. et al. 2019. The anti-mycobacterial activity of a diterpenoid-like molecule operates through nitrogen and amino acid starvation. Frontiers in Microbiology 10 1444. (10.3389/fmicb.2019.01444)
- Crusco, A. et al. 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)
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Websites
- Edwards, D. et al. 2022. A rapid scoping review of harm reduction strategies for ecstasy (MDMA) users in recreational settings. [Online].Research Square: Research Square. (10.21203/rs.3.rs-2178425/v1)Available at: https://doi.org/10.21203/rs.3.rs-2178425/v1.
Research
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:
- Targeted drug discovery in advanced/metastatic colorectal and breast cancer (Bcl-3 inhibition)
- Targeting cancer stem cells for selective apoptosis induction (c-Flip inhibition)
- 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 that progressed to clinical trial (Phortress). Other recent research activities include:
- Targeted protein degradation (PROTACs) as a therapeutic approach in cancer therapy
- Protein-protein interaction targets in cancer
- Selective induction of apoptosis in cancer cells
- Diagnostic imaging (18F radiochemistry) in cancer using Positron Emission Tomography (PET).
- Characterisation of novel psychoactive substances (WEDINOS Project), carried out in conjunction with Public Health Wales and Cardiff & Vale University Health Board (Llandough Hospital).
Collaborators
Cardiff University
- Prof. Richard Clarkson (School of Biosciences)
- Prof. Arwyn Jones (School of Pharmacy and Pharmaceutical Sciences)
External
- Prof. Andrea Brancale (University of Chemistry and Technology, Prague)
- Dean Acreman, Rick Lines, 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 drug characterisation
Current research funding
- 2024-6 Cancer Research Wales: Development of new PROTACs (PDRA: Dr. Dusan Ruzic)
- 2025-8 Myristica Trust: New BCL3 inhibitors (PhD studentship: Tia Elstow)
- 2012- Public Health Wales (Welsh Government) / NHS Wales: New Psychoactive Substances Project – Action in Wales. Contribution: drug analysis by NMR spectroscopy.
Teaching
- PH3115 Optimisation of drug design
- PH4116 Pharmacy research or scholarship project (module managment team)
- PH4117 Pharmaceutical sciences, pharmacy practice and the population (module leader)
Biography
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, and Professor in 2016.
Scientific and professional service
I serve as an Independent Board member (University) for the Velindre University NHS Trust (since August 2021).
I chair the management board for the Cardiff Medicentre (https://www.cardiff.ac.uk/medicentre), a joint venture between Cardiff University and Cardiff & Vale University Health Board.
I am 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.
I am an Honorary Professor at Amity University (Uttar Pradesh, India), within the Amity Institute of Molecular Medicine & Stem Cell Research
Prizes / membership of professional bodies
-
Royal Society of Chemistry Malcolm Campbell memorial prize winner 2003 (with MFG Stevens and TD Bradshaw).
- Member of the British and European Associations for Cancer Research (BACR & EACR).
- I serve as a scientific board member for the PAMM (Pharmacology and Molecular Mechanisms) group, a laboratory division of the EORTC.
Contact Details
Research themes
Specialisms
- Medicinal and biomolecular chemistry