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Associate Professor Brian W DYMOCK

BSc (Hons), University of Strathclyde
PhD, University of Glasgow

Department of Pharmacy, National University of Singapore
18 Science Drive 4, Singapore 117543
Tel: +65 6601 2495
Fax: +65 6779 1554
Email: phadbw@nus.edu.sg
Research Group

  • PR1101 Physicochemical Principles Of Drug Action (Practical)
  • PR5212: Advanced Topics in Medicinal Chemistry
  • PR4105: Natural Products (Practical)
  • PR4205: Bioorganic Principles of Medicinal Chemistry

Throughout my 15 year industrial career I have worked on a wide variety of medicinal chemistry and drug development projects across a spectrum of industry. My experience includes discovery of leads and development of them into clinical candidates using organic synthesis, analytical chemistry, structure-based design (use of X-ray structures and computational chemistry to progress lead candidates), analysis of multi-disciplinary structure activity relationships (SAR), progression of compounds through hit to lead and lead optimization, pre-clinical development, CMC management for GMP API material for clinical trials, CMC regulatory and quality for API. Intellectual property – extensive experience of patent drafting for composition of matter, use and solid form patents.

 

In NUS I plan to bring industry ‘best practices’ to Academic Drug Discovery through the NUS Drug Development Unit (DDU) and through specific collaborations with like-minded colleagues.

 

Specific areas of experience include:

  • Medicinal Chemistry of enzyme inhibitors and modulators of receptors and ion channels.
  • Fragment Screening for Lead Identification for start-points for medicinal chemistry.
  • Structure-based design for progression of medicinal chemistry lead series.
  • Synthetic route development towards biologically active compounds.

 

Selected publications available here.

Kinase Inhibitors for cancer and autoimmune disease, particularly inhibitors of JAK2, FLT3, CDKs, PI3Ks, mTOR, PDK1, HDAC and HMTs.
Chaperone Inhibitors, particularly, Hsp90.
Protease inhibitors, particularly, anti virals for Hepatitis C (NS3 protease) and HIV (Reverse Transcriptase).
Anti-bacterials and application of medicinal chemistry to CNS diseases.

 

Specific Therapeutic contributions, as a member of a multidisciplinary team:

  • NVP-AUY922, Hsp90 inhibitor, licensed to Novartis and now in Phase 2 clinical trials for cancer
  • BEP800, Hsp90 inhibitor discovered through Fragment Screening, licensed to Novartis.
  • Pacritinib (SB1518) – JAK2/FLT3 kinase inhibitor for cancer, licensed to Cell Therapeutics, now in Phase 3
  • SB1578 – JAK2/FLT3 kinase inhibitor for autoimmune diseases (e.g. Rheumatoid Arthritis), licensed to Cell Therapeutics
  • SB1317 – CDK/JAK/FLT3 inhibitor for serious cancers (e.g. acute leukemia), licensed to Tragara Pharmaceuticals, in Phase 1
  • Pracinostat (SB939) – a pan-HDAC inhibitor for cancer, licensed to MEI Pharma, in Phase 2
  • SB2343 – selective mTOR/pan-PI3K inhibitor for cancer, licensed to Verastem
  • SB2602 – selective mTOR inhibitor for cancer and non-oncology indications