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Dr Ketan Ruparelia

Job: Research Assistant

Faculty: Health and Life Sciences

School/department: Leicester School of Pharmacy

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

T: +44 (0) 1162 57 7283

E: kruparel@dmu.ac.uk

W: www.dmu.ac.uk/hls

 

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: 

  • The design, synthesis and optimisation of tumour selective anti-cancer agents
  • 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

Research group affiliations

Natural Products Research Group (Dr Arroo),

The Molecular Toxicology Group (Prof Bob Chaudhuri).

Publications and outputs 

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

Research interests/expertise

Anti-Cancer Research: Tumour selective drug design, multi scale synthesis for biological evaluation. PhD thesis title, ‘Synthesis of Novel CYP1-activated Anti-cancer Prodrugs’. Area of study: Design, Synthesis and Optimisation for in-vitro biological evaluation of reference and novel small-molecules for cytochrome P450 CYP1-enzyme targeted prodrug cancer chemotherapy.

This includes the design and synthesis of novel prodrugs targeted towards CYP1B1, an aromatic hydroxylase specifically expressed in all tumour samples investigated to date, but not in normal somatic tissues.

The development of prodrugs is based partly on the structure of natural product, Estradiol, a known substrate of CYP1B1 activation to partly toxic 4-hydroxyestradiol.

Purification by flash column chromatography or recrystallisation and analytical techniques include 1H and 13C NMR, mass spectrometry and infrared spectra analysis.

Qualifications

BSc, MSc, PhD

Honours and awards

PhD in Medicinal Chemistry (Graduated summer 2011).

Membership of external committees

Since 2005-present:

  • British Association for Cancer Research (BACR)
  • European Association for Cancer Research (EACR)
  • Phytochemical Society of Europe
  • British Mass Spectrometry Society (BMSS)
  • The Royal Society of Chemistry (RSC)
  • The Academy of Pharmaceutical Sciences of Great Britain.

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’

Case studies

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 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.

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.

Examples of evidence of the ‘impact’ of research e.g. references to reviews / articles in main stream media, examples of feedback from users, exhibition attendance figures.

Ketan Ruparella

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