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Progress in Medicinal Chemistry - 1st Edition - ISBN: 9780444634801, 9780444634856

Progress in Medicinal Chemistry, Volume 54

1st Edition

Serial Editors: G. Lawton David Witty
Hardcover ISBN: 9780444634801
eBook ISBN: 9780444634856
Imprint: Elsevier
Published Date: 30th January 2015
Page Count: 314
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Table of Contents

Chapter One: Recent Advances in Cancer Therapeutics

  • Abstract
  • 1 Introduction
  • 2 Chaperone Inhibitors
  • 3 Kinase Inhibitors
  • 4 HDAC Inhibitors
  • 5 Inhibitors of Protein-Protein Interactions (PPIs)

Chapter Two: Fluorine in Medicinal Chemistry

  • Abstract
  • 1 Introduction
  • 2 Survey of Fluorine Chemotypes in Marketed Drugs
  • 3 Impact of Fluorine on Lipophilicity
  • 4 Impact of Fluorine on pKa
  • 5 Impact of Fluorine on Metabolism
  • 6 Metabolism to Toxic Metabolites
  • 7 Fluorine Interactions in Proteins
  • 8 Conformational Influences of Fluorine
  • 9 Marketed Drug Case Studies
  • 10 Summary and Future Outlook

Chapter Three: A Perspective on the Next Generation of Antibacterial Agents Derived by Manipulation of Natural Products

  • Abstract
  • 1 Introduction
  • 2 Glycopeptides
  • 3 Tetracyclines
  • 4 Aminoglycosides
  • 5 Ketolides
  • 6 Thiazolyl Peptides
  • 7 Pleuromutilins
  • 8 Polymyxins
  • 9 Conclusion

Chapter Four: A New Era for Chagas Disease Drug Discovery?

  • Abstract
  • 1 Introduction
  • 2 Benznidazole as Historic Anti-Chagasic Chemotherapy
  • 3 CYP51 as a Drug Target for T. cruzi Growth Inhibition
  • 4 Clinical Trials
  • 5 Evolution of Screening Cascades
  • 6 Compound Landscape for Chagas Disease Chemotherapies
  • 7 Summary

Chapter Five: Imaging in Drug Development

  • Abstract
  • 1 Introduction
  • 2 Magnetic Resonance Imaging
  • 3 Nuclear Medicine Imaging
  • 4 Summary and Future Prospects


Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume includes chapters covering recent advances in cancer therapeutics,  fluorine in medicinal chemistry, a  perspective on the next generation of antibacterial agents derived by manipulation of natural products, a  new era for Chagas Disease drug discovery? and imaging in drug development.

Key Features

  • Extended timely reviews of topics in medicinal chemistry
  • Targets and technologies relevant to the discovery of tomorrow’s drugs
  • Analyses of successful drug discovery programmes


Everyone interested in the strategy and practice of the preclinical phases of the creation of new medicines. Those wishing to understand the drivers of drug design or expand their knowledge of therapeutic target classes


No. of pages:
© Elsevier 2015
30th January 2015
Hardcover ISBN:
eBook ISBN:

Ratings and Reviews

About the Serial Editors

G. Lawton

G. Lawton

Dr Geoff Lawton has extensive experience in new medicine discovery across many therapeutic areas in both large and small companies and is a co-inventor of a marketed drug (Cilazapril). He is a former Director of Chemistry at Roche UK, and Vice-president Chemistry and Preclinical Sciences within Roche Bioscience, Palo Alto, USA. He was for five years the research member of a global therapy area strategy planning team for inflammatory diseases, aligning research with the clinical development and marketing parts of the business.

From 2003 to 2007 he was founding Research Director with Lectus Therapeutics building from start-up a drug discovery organisation; generating the team, facilities and project portfolio targeting the next generation of ion channel modulating medicines.

Since 2001 Geoff has provided scientific and strategic evaluation and advice on drug discovery as an independent consultant for a number small and medium sized biotech companies, CROs, VCs, academic groups and medical research charities.

Geoff serves on the Board of Antabio, a French biotech company developing tomorrow’s antibacterial drugs.

He is a founder of INMedD, a new medicines discovery social enterprise.

Affiliations and Expertise

St. Ippolyts, Herts, UK

David Witty

David Witty

Dr David Witty has more than 20 years experience in the pharmaceutical industry as a medicinal chemist and project leader working principally in areas of anti-infectives, metabolic diseases, cognition and pain, delivering clinical candidates for several conditions. He led IT Strategy within the Neurology division of GSK, developing and deploying the first Electronic Notebooks for drug discovery to sites in the UK and Singapore. He has contributed more than 90 scientific papers, reviews, patents and books on medicinal and synthetic chemistry.

In 2010 David and several colleagues successfully raised $35M in venture funding to found Convergence Pharmaceuticals, a specialist ion channel company focused on the development of novel treatments for pain, based in Cambridge UK. David presently leads their discovery programme and manages scientific operations within the business.

David is chairman of the Fine Chemicals Group of the Society of Chemical Industry, with responsibility for the delivery of conferences, seminars and training courses for chemists throughout the UK and Europe, and advising parliamentary bodies on matters of relevance to the UK chemical industry.

Since 2008 David has been a STEM ambassador for SETPOINT, introducing school students at both primary and secondary level to the excitement and possibilities of pursuing scientific careers, through workshops, lectures and competitions.

Affiliations and Expertise

WITNET LTD, Cambridge, UK