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Dr Ketan. C, Ruparelia

Job: Researcher and Part-Time Lecturer

Faculty: Health and Life Sciences

School/department: Leicester School of Pharmacy

Address: De Montfort University, The Gateway, Leicester, LE1 9BH.

T: +44 (0) 116 257 7283

E: kruparel@dmu.ac.uk

W: https://dmusquaremile.our.dmu.ac.uk/health-and-wellbeing/

Social Media: www.atiner.gr/

 

Personal profile

Achievements

  • Anti-Cancer research publications and national and international conference presentations
  • Synthesised and optimised a novel, patented anti-tumour agent BanoxantroneTM {AQ4N}, currently in Phase III Clinical Trials
  • Prepared a unique DNA-affinic probe, DRAQ5TM commercialised via  (www.Biostatus.com)
  • Synthesised and optimised a potential CYP1-activated anti-cancer agent StilsereneTM (DMU 212) currently at pre-clinical stage (national press and media coverage in July 2001; Cancer Drug Discovery Group)
  • Medicinal Chemistry Research Laboratory Safety Manager
  • Complete redesign, organisation and management of Medicinal Chemistry Research Laboratory in Cancer Drug Discovery Group

Professional Experience

  • 20 years management of Medicinal Chemistry Research Laboratory
  • 8 years research experience in multiscale synthesis of DNA affinic anti-tumour agents
  • 12 years expertise in small-molecule laboratory synthesis for enzyme targeted pro-drug cancer chemotherapy
  • Working knowledge of health and safety, broad experience of risk assessments under Control of Substances Hazardous to Health [COSHH] regulations (1990), data protection and auditing procedures
  • Analytical [(Nuclear Magnetic Resonance; Bruker AC 400MHz), MALDI-Lasermat 2000 Mass Spectrometry, Infra-red Spectroscopy (Perkin Elmer FTIR); UV DU70 Beckman technical; equipment and IT databases, Isis Draw 2.4, Isis Base, GraphPad Prism version 3.00 and Endnote.
  • Purification techniques: flash column chromatography, recrystallisation, high-vacuum distillation, trituration, precipitation.
  • Solid and solution phase combinatorial chemistry

Personal Profile: 

  • Design, synthesis, optimisation & biological evaluation of potential agents (chalcones, stilbenes, flavones analogues) and natural products for cancer, diabetes, neglected tropical diseases and antimicrobial therapies
  • Prodrug activation mechanisms
  • Tumour activated apoptosis induction
  • Tumour activated antimitotic agents
  • Dietary cancer chemopreventative agents
  • Human cell culture
  • Combinatorial chemistry
  • Natural products isolation as anti-cancer agents

LinkedIn Profile 
https://www.linkedin.com/in/ketanruparelia/

ResearchGate 
https://www.researchgate.net/profile/Ketan_Ruparelia

Research group affiliations

  • Chemistry for health
  • Natural Products Research Group
  • The Molecular Toxicology Group
  • Pharmaceutical Technologies

Publications and outputs 

Click here for a full listing of Ketan Ruparelia‘s publications and outputs.

Research interests/expertise

  • Design, synthesis & biological evaluation of potential agents (chalcones, stilbenes, flavones analogues) and natural products for cancer, diabetes, neglected tropical diseases and antimicrobial therapies
  • Medicinal Chemistry
  • Natural Product Isolation
  • Heterocyclic Chemistry
  • Phytotherapy
  • Analytical Chemistry

Qualifications

  • BSc (Hons)
  • PhD
  • PGCert
  • MRSC
  • Fellow of the Higher Education

Courses taught

  • Pharmacy
  • Biomedical Science
  • Pharmaceutical and Cosmetic Sciences
  • Forensic Science
  • Chemistry of medicinal natural products
  • Phytotherapy, complementary and alternative medicine
  • Professional and Scientific Skills
  • Bioanalysis, Pharmaceuticals and Health (BPH) Doctoral Training Programme (teaching assistant)
  • Research projects

Honours and awards

  • OSCAR Award Finalist 2017- Outstanding Contribution to Promoting our City
  • Visiting Professors: one of nine selected on the activities related to the international Programmes of the University of L’Aquila, Italy (http://www.univaq.it/en/section.php?id=1794 
  • Diabetes UK Inspire Awards nomination for Campaigning and Raising Awareness Award category for the DMU Square Mile Diabetes Health Awareness Project (2016)
  • The Times Higher Education Leadership and Management Awards (THELMAs) 2015; Shortlisted; Knowledge Exchange/Transfer Initiative of the Year-DMU Square Mile Diabetes Health Project
  • DMU Oscar Finalist Award 2015 for Outstanding Contribution to the Public Good (Square Mile Diabetes Project nominated by Square Mile Team)
  • DMU Oscar Finalist Award 2014 for Outstanding Contribution to the Public Good _Square Mile Diabetes Project
  • DMU Oscar nomination for Outstanding Contribution to Research and Innovation-2014
  • DMU-Square Mile Diabetes Health Awareness project shortlisted and finalist for ‘     THE AWARDS Research 2014 Project of the Year
  • Awarded Outstanding Contribution to Research Excellence (OSCAR) presented by Professor Andy Collop at De Montfort University (July 2012)

Membership of external committees

Head, Pharmaceutical Research Unit, Pharmaceutical Sciences: Athens Institute for Education & Research ATINER (2016-present) https://www.atiner.gr/

Membership of professional associations and societies

  • Royal Society of Chemistry
  • Phytochemical Society of Europe
  • Academy of Pharmaceutical Sciences GB (APSGB)
  • Fellow of the Higher Education Academy
  • British Association for Cancer Research (BACR)
  • European Association for Cancer Research (EACR)
  • British Mass Spectrometry Society (BMSS)
  • Academic Member of Athens Institute for Education and Research ATINER (https://www.atiner.gr/)

Professional licences and certificates

  • Diabetes UK professionally trained Community Champions to raise awareness of the risk factors of Type 2 diabetes and provide information, including signposting them to local services, to help prevent them from developing the condition, or if they already have it to help them manage it.
  • Certificate in Research Supervision

Conference attendance

Health and Wellbeing Research Showcase 23 June 2011, De Montfort University, Leicester; Poster presentation: “A Smart Bullet to Target Breast Cancer – Stilserene (DMU 212) http://www.dmu.ac.uk/research/research-highlights/health-and-wellbeing/

Phytochemical Society of Europe International Symposium: Trends in Natural Products Research, 11-14 April 2010, De Montfort University, Leicester (ISBN 978-0-9565402-0-0); Poster and short lecture: ‘Artemisinin-Chalcone hybrid preparation as potential anti-tumour prodrugs’

National Science and Engineering Week (Science, Engineering and Technology 2009; SET for BRITAIN 2009), 9-3-2009 House of Commons Terrace Marguee; Poster presentation: ’A Smart Bullet to Target Breast Cancer’

Phytochemical Society of Europe (PSE) International Symposium on Natural Products in Cancer Therapy 23-26 Sept 2008. Naples, Italy; Poster presentation: ‘Purification, Characterisation & Metabolite Synthesis of Nobiletin and Tangeretin’

UK GRAD Midland Hub Poster Competition (23 April 2008; Prize: Best Poster: 'A Smart Bullet to Target Breast Cancer – Stilserene' (DMU 212)

National Organic Symposium Trust (NOST); 3rd NOST Conference for Research Scholars, 15-18 November 2007, Guru Nanak Dev University, Amritsar, India. Short lecture: ‘The Design and Synthesis of CYP-activated Anti-cancer Prodrugs’

Consultancy work

  • British Technology Group (BTG)-development of BanoxantroneTM (AQ4N) and precursors (1998)
  • Research programme: CYP1-activated cancer therapy - Spear Therapeutics (Scaled synthesis of StilsereneTM and its potential CYP1-activated metabolites (2001) 

Current research students

Supervising 4 PhD students

Please contact for MSc or PhD opportunities.

Internally funded research project information

  • HEIF-Synthesis of Novel Antiprotozoal Agents for the Treatment of Neglected Tropical Diseases (Jointly funded) -£25K (2013)
  • Joint HEIF -DNA tests for toxic weed contamination of herbal medicines (Jointly funded) -£14.5K (2016)

Published patents

Novel compounds for Human African Trypanosomiasis (sleeping sickness). UK. Patent Application Number 1400366.9.

Professional esteem indicators

Academic Head of Pharmaceutical Research Unit, ATINER and jointly responsible for the conferences:

  • 4th Annual International Conference on Health & Medical Sciences & 2nd Annual International Symposium on Diabetes; 2-5 May 2016, Athens, Greece
  • 5th Annual International Conference on Health & Medical Sciences & 3rd Annual International Symposium on Diabetes 1-4 May 2017, Athens, Greece”

 

Case studies

  1. The synthesis of novel bioreductive anti-cancer agents and the consequent discovery of anthraquinone derivative AQ4N, (BanoxantroneTM) that is currently in Phase III clinical trials for oesophageal cancer (led by Prof LH Patterson). The intellectual property and technology commercialisation company British Technology Group (BTG) originally supported the development of AQ4N.Kudos acquired a worldwide license for AQ4N from BTG in March 2001 and is developing this in collaboration with Novacea; AQ4N is a radiation therapy enhancer and chemotherapy sensitizer.

  2. Synthesised a novel patented agent, DRAQ5TM and is now supplied exclusively for in-vitro research purposes only as cellular DNA fluorescent stain by Biostatus Limited UK (www.biostatus.com). DRAQ5™ is a pure synthetic compound with high affinity for DNA; stable at room temperature; stable under normal lighting conditions and soluble in water at biologically compatible Ph 

  3. Synthesised and optimised a potential cytochrome P450 CYP1-activated anti-cancer agent StilsereneTM (DMU 212) currently at preclinical stage. (national press and media coverage in July 2001)

    1. https://www.slideshare.net/gerrypotter52/breakthroughs-in-the-quest-to-cure-cancer

  4. Innovative partnership between DMU and Louisville Kentucky USA (A key focus will be diabetes, which is a major health issue in both Leicester and Louisville (2016). DMU students have been working with Diabetes UK to train as community champions, helping to identify those potentially at risk and referring them to General Practioners

    1. http://www.louisvilledistilled.com/innovationnews/citycollaborativedemontfortu.aspx

  5. A knowledge transfer partnership 2015-2018 between De Montfort University and Diabetes UK directly result  of DMU student-led DMU-Square Mile Diabetes Health Awareness project.

    1. http://www.dmu.ac.uk/about-dmu/news/2016/february/students-launch-pioneering-partnership-with-diabetes-uk.aspx
    2. http://m.leicestermercury.co.uk/Students-train-help-spot-diabetes-risk/story-28892192-detail/story.html
    3. http://www.dmu.ac.uk/about-dmu/news/2015/november/dmu-students-ready-to-help-transform-leicester-with-dmulocal.aspx
    4. https://dmusquaremile.our.dmu.ac.uk/2015/09/19/know-your-risk-with-our-diabetes-uk-community-champions/ 

  6. A first move in a knowledge transfer partnership of diabetes awareness project between De Montfort University and University of L’Aquila in central Italy to help to set up a similar project, to try and tackle the country’s diabetes problem, dealing with which costs the nation $12 billion as part of the European Research Street Science  

    1. http://www.dmu.ac.uk/about-dmu/news/2015/april/dmu-team-shares-pioneering-research-with-italian-university.aspx; http://dmulocal.dmu.ac.uk/news-listing/italian-student-takes-dmulocal-diabetes-teaching-overseas/ 

  7. The DMU-Square Mile Diabetes Health Project successfully launched an official partnership with national charity Diabetes UK to tackle one of largest and current health issues affecting Leicester. De Montfort University and Diabetes UK are working together to diminish barriers and further enhance the delivery of diabetes care to the communities throughout Leicester. This pioneering partnership has enabled 47 DMU students to complete high-quality training to become certified Diabetes UK Community Champions. The students are qualified to assess and identify individual’s risk of developing type 2 diabetes and consequently refer members of the public to their GP’s. Furthermore, the students have the ability and understanding to offer substantial information and guidance regarding diabetes prevention strategies, thus raising awareness of the condition to educate others. The 47 DMU Community Champions have supported 42 separate events and effectively engaged with 3,281 individuals across Leicester city. 1,530 of the entire figure have been identified as pupils from 6 different local schools who participated in interactive diabetes awareness assemblies. The remaining 1,751 individuals represented the public who partook in various collaborative events hosted by local partners such as St Matthews Library, Highfields Centre and Belgrave Neighbourhood Centre. 373 people out of the 1,751 received guidance, information and Know Your Risk assessments from the dedicated DMU Community Champions. Diabetes UK Community Champion Project 2016/17: 159 DMU students have been trained as DUK Community Champion’s. Of this overall number, we currently have 125 active DUK CC volunteers who attend a wide range of events across the community, focusing on BME demographics, to raise awareness of diabetes, type 1, type 2, diet, exercise and risk assess individuals to identify their possibility of contracting type 2 diabetes.  

Conference presentations and publications

1. Science Without Borders International Presentation; XXI Semana de Ciência, Tecnologia e Cultura (CIENTEC 2015) (XXI Week of Science, Technology and Culture); Universidad Federal do Rio Grande do Norte (Federal University of Rio Grande do Norte); Natal, RN –Brazil; 20-23rd October 2015 "Síntese e avaliação da atividade antimicrobiana e antioxidante de chalconas derivadas da combretastatina" (Synthesis and evaluation of antimicrobial and antioxidant activity of combretastatin-like chalcones) Renata de Carvalho Feitosa; Ketan Ruparelia

2. Athens Institute For Education and Research (ATINER): 2nd Annual International Conference on Pharmaceutical Sciences, 4-7 May 2015, Athens, Greece; Plenary Presentation ‘Resveratrol and Synthetic Analogues: From Cardioprotective Effects to Anticancer Activities http://www.atiner.gr/pharmako 

3. Phytochemical Society of Europe International Symposium: Trends in Natural Products; Research, 23rd -25th June 2014, Olomouc, Czech Republic. Abstract, poster (ISBN 978-0-9565402-0-0): ‘An Extraction, Purification and Characterisation of the lignans Podophyllotoxin and β-Peltatin from Podophyllum peltatum.

Poster presentation: “An Extraction, Purification and Characterisation of the lignans Podophyllotoxin and β-Peltatin from Podophyllum peltatum”

4. Phytochemical Society of Europe 2nd International Symposium: Natural Products in Cancer Prevention and Therapy; Trends in Natural Products Research, 25th - 28th June 2013, Naples, Italy. Abstract, poster and short lecture (ISBN -13978-0-9565472-2-4): http://www.phytochemicalsociety.org/naples/

Effects of a Natural Extract of Chestnut Wood (Castanea sativa Mill.) rich in ellagitannins, with anticancer effects, towards cardiovascular system

“Isolation, purification and identification of Crocin and Kaempferol, powerful antioxidants, in Crocus sativus L. Flowers

“Phytoestrogens as Natural Prodrugs in Cancer Prevention: towards a Mechanistic model”

5. Phytochemical Society of Europe International Symposium: Trends in Natural Products

Research, 11th -14th April 2010, De Montfort University, Leicester. Abstract, poster and short lecture (ISBN 978-0-9565402-0-0): ‘Artemisinin-Chalcone hybrid preparation as potential antitumor prodrugs’.

6. Science, Engineering and Technology (SET), 9th March 2009 at the House of Commons Terrace Marguee. Poster presentation: ‘A Smart Bullet to Target Breast Cancer’.

7. Phytochemical Society of Europe International Symposium: Natural Products in Cancer Therapy, 23rd-26th September 2008, Naples, Italy. Poster presentation: ‘Purification, Characterization & Metabolite Synthesis of Nobiletin and Tangeretin’.

8. UK GRAD Midland Hub Poster Competition, 23 rd April 2008, De Montfort University, Leicester. Best poster prize: ‘Stilserene (DMU 212)-A smart bullet to Target Breast Cancer’.

9. National Organic Symposium Trust (NOST); 3rd NOST Conference for Research Scholars, 15th-18th November 2007, Guru Nanak Dev University, Amritsar, India. Short lecture: ‘The Design and Synthesis of CYP-activated Anticancer Prodrugs’.

10. M.R.Craven, L.H. Patterson, K. C. Ruparelia (1992) Use of N-oxides of DNA affinic anthraquinones as bioreductive prodrugs. Annals of Oncology. 3 (1), 94. Poster presented at the seventh NCI/EORTC meeting on New Drugs in Cancer Therapy, Amsterdam (Mar. 1992).

11. M.R.Craven, G.R.Fisher, L.H. Patterson, K. C. Ruparelia (1992) N-oxides of DNA affinic agents as bioreductive activated prodrugs. Proceedings of the 83rd Annual Meeting of the American Association of Cancer Research, San Diego, USA (May 1992). Published in Proc Am Assoc Cancer Res., (33),

12. M.R.Craven, L.H. Patterson, K. Ruparelia (1993) Activity of novel anthraquinone-N-oxide prodrug DNA binding agents against murine colon adenocarcinomas in vivo. The PAMM Winter Meeting, Pharmacogenetic and Anticancer drug metabolism, France (Jan. 1993)

13. M.R.Craven, L.H. Patterson, K. Ruparelia (1993) Activity of novel anthraquinone-N-oxide prodrug DNA binding agents against murine colon adenocarcinomas in vivo. The British Association for Cancer Research, Sheffield (Mar. 1993). Published in Brit J Cancer, 67(S20) 85.

14. M.R.Craven, L.H. Patterson, K. Ruparelia (1993) Aliphatic N-oxides as prodrug DNA binding agents: a new class of bioreductive activated antitumour agent. 8th International Conference on Chemical Modifiers of Cancer Treatment, Kyoto, Japan (Jun. 1993)

15. Y. Giles, M. Craven, L.H.Patterson, K.Ruparelia, P. Teesdale-Spittle (1994) Relationship between DNA binding affinity, inhibition of Topoisomerase II and cytotoxicity of some novel alkylaminoanthraquinone antitumour agents: development of prodrugs. The British Pharmaceutical Conference, London (Sept. 1994). J Pharm Pharmac 1994

16. Y. Giles, M. Craven, L.H.Patterson, K.Ruparelia, P. Teesdale-Spittle (1994) N-oxides of alkylaminoanthraquinone antitumour agents as prodrug Topoisomerase II inhibitors. International Meeting on Medicinal Chemistry, Bath, UK (Sept. 1994)

17. L. Hoon, P.J. Perry, G.A. Potter, K. Ruparelia (1999) Design and Synthesis of Aromatic Prodrugs for Cancer Chemotherapy. De Montfort University, Leicester (Sept. 1999)

18. T. M. El-Gogary, L. H. Patterson, K. Ruparelia, P. Teesdale-Spittle, M. I. Needham (2001) Charge-Transfer Complexes of some Models of DNA-Affinic Agents. COMPUTER CHEMISTRY CENTER University of Erlangen, Germany

19. Interaction of anthraquinone anti-cancer drugs with DNA. Tarek M. El-Gogary1, Laurence H. Patterson, Ketan Ruparelia, Paul Teesdale-Spittle, Michael I. Needham and M. S. Soliman School of Chemistry, University of Bristol, Bristol BS8 1TS, UK

20. Potter, G.A., Patterson, L.H., Wanogho, E., Perry, P.J., Butler, P.C., Ijaz, T., Ruparelia, K.C., Wilsher, N.E., Stanley, L.A. and Burke, M.D. (2001) Human cytochrome P450 CYP1B1 metabolises the natural cancer preventative compound, resveratrol, to the anticancer agent, piceatannol. Drug Met Rev 33 (Suppl 1), 83.

21. Potter, G.A., Patterson, L.H., Wanogho, E., Perry, P.J., Butler, P.C., Ijaz, T., Ruparelia, K.C., Wilsher, N.E., Stanley L.A. and Burke, M.D. (2001) Metabolism of the natural cancer preventative agent resveratrol to the anticancer agent piceatannol by cytochrome P450 CYP1B1. 153. In: British Pharmaceutical Conference Proceedings 2001. Pharmaceutical Press. (ISBN: 0-85369-512-1).

22. Potter, G.A., Butler, P.C., Ruparelia, K.C., Ijaz, T., Wilsher, N.E., Wanogho, E., Tan, H.L., Hoang, T.T.V., Stanley, L.A. and Burke, M.D. (2002) DMU-212: A novel CYP1B1 activated anticancer prodrug. Brit J Cancer 86 (Suppl. 1), S117.

23. Wilsher, N.E, Butler, P.C., Ijaz, T., Ruparelia, K.C., Tan, H.L., Wanogho, E., Burke, M.D. and Potter, G.A. (2003) Selective metabolism of resveratrol by human CYP1 family isozymes. J Chemother 15 (Suppl. 1), 108.

24. Butler, P.C., Ruparelia, K.C., Ijaz, T., Tan, H.L., Wilsher, N.E., Perry, P.J., Burke, M.D. and Potter, G.A. (2003) DMU-135: A CYP1B1 activated tyrosine kinase inhibitor prodrug with tumour selective activity. Brit J Cancer 87 (Suppl. 1), S33.

25. Pors K, Paniwnyk Z, Ruparelia KC, Teesdale-Spittle PH, Hartley JA, Kelland LR, Patterson LH. 2004. Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumour cells. J Med Chem.;47(7):1856-9

26. Sale S, Tunstall RG, Ruparelia KC, Potter GA, Steward WP, Gescher AJComparison of the effects of the chemopreventive agent resveratrol and its synthetic analog trans 3,4,5,4 '-tetramethoxystilbene (DMU-212) on adenoma development in the Apc(Min+) mouse and cyclooxygenase-2 in human-derived colon cancer cells. INTERNATIONAL JOURNAL OF CANCER 115 (2): 194-201 JUN 10 2005

27. Sale S, Verschoyle RD, Boocock D, Ruparelia KC. Pharmacokinetics in mice and growth-inhibitory properties of the putative cancer chemopreventive agent resveratrol and the synthetic analogue trans 3,4,5,4 '-tetramethoxystilbene . BRITISH JOURNAL OF CANCER 90 (3): 736-744 FEB 9 2004

Acknowledgements in publication for technical excellence

  • L.H. Patterson (1993) Rationale for the use of aliphatic N-oxides of cytotoxic anthraquinones as prodrug DNA-binding agents- a new class of bioreductive agent. Cancer Metastas Rev 12, 119-134
  • M.R. Craven, G.R. Fisher, P. Teesdale-Spittle (1994) Aliphatic amine N-oxides of DNA-binding agents as bioreductive drugs. Oncol Res 6, 533-538
  • M.V. Hejmadi, L.H. Patterson (1995) AQ4N- an alkylaminoanthraquinone N-oxide showing bioreductive potential and positive interaction with radiation in vivo. Brit. J. Cancer 72, 76-81. 

Joint collaboration

International research collaboration

  • Prof. Stefania A. Nottola, Associate Professor of AnatomyDepartment of Anatomy, Histology, Forensic Medicine and Orthopaedics, Electron Microscopy Unit, Laboratory "Pietro M. Motta" Faculty of Pharmacy and Medicine, University of Rome La Sapienza, Via Alfonso Borelli 50, Rome 00161, Italy
  • Prof. Macchiarelli, Prof. Maria A. Continenza (Department of Life, Health and Environmental Sciences - University of L’Aquila), Dr Keti Zeka( Department of Industrial and Information Engineering and Economics - University of L’Aquila, Via G. Gronchi 18, L’Aquila, Italy
  • Dr Vasilis Androutsopoulos, Laboratory of Toxicology, University of Crete, Medical School Voutes, GR-71110 HERAKLON, GREECE
  • University of Bologna (Prof. Roberta Budriesi; Dr Micucci Matteo), Dip. Scienze Farmaceutiche, Alma Mater Studiorum Università di Bologna via Belmeloro, 6, 40126, Bologna 

#DMUGlobal Faculty led trips

DMU Global Faculty led Trip with PhD students from School of Pharmacy to Copenhagen 2016 (9th Joint Natural Products Conference 2016 in Copenhagen - a joint conference organized by University of Copenhagen, http://www.conferencemanager.dk/JointNaturalProductsConference2016/home.html)

International Collaborations

Ketan Ruparella

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