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El. knyga: Progress in Medicinal Chemistry

Series edited by (St. Ippolyts, Herts, UK), Series edited by (WITNET LTD, Cambridge, UK)
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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.


    • 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

    Daugiau informacijos

    A review of eclectic developments in medicinal chemistry, with authoritative extended reviews of targets and technologies addressing new therapeutics
    Contributors vii
    Preface ix
    1 Recent Advances in Cancer Therapeutics
    1(64)
    Nicola Chessum
    Keith Jones
    Elisa Pasqua
    Michael Tucker
    1 Introduction
    1(1)
    2 Chaperone Inhibitors
    2(10)
    3 Kinase Inhibitors
    12(20)
    4 HDAC Inhibitors
    32(9)
    5 Inhibitors of Protein-Protein Interactions (PPIs)
    41(24)
    References
    54(11)
    2 Fluorine in Medicinal Chemistry
    65(70)
    Steven Swallow
    1 Introduction
    66(1)
    2 Survey of Fluorine Chemotypes in Marketed Drugs
    67(2)
    3 Impact of Fluorine on Lipophilicity
    69(4)
    4 Impact of Fluorine on pKa
    73(10)
    5 Impact of Fluorine on Metabolism
    83(5)
    6 Metabolism to Toxic Metabolites
    88(3)
    7 Fluorine Interactions in Proteins
    91(3)
    8 Conformational Influences of Fluorine
    94(7)
    9 Marketed Drug Case Studies
    101(24)
    10 Summary and Future Outlook
    125(10)
    References
    126(9)
    3 A Perspective on the Next Generation of Antibacterial Agents Derived by Manipulation of Natural Products
    135(50)
    Pamela Brown
    Michael J. Dawson
    1 Introduction
    135(2)
    2 Glycopeptides
    137(6)
    3 Tetracyclines
    143(7)
    4 Aminoglycosides
    150(7)
    5 Ketolides
    157(4)
    6 Thiazolyl Peptides
    161(5)
    7 Pleuromutilins
    166(5)
    8 Polymyxins
    171(7)
    9 Conclusion
    178(7)
    References
    178(7)
    4 A New Era for Chagas Disease Drug Discovery?
    185(46)
    Martine Keenan
    Jason H. Chaplin
    1 Introduction
    185(2)
    2 Benznidazole as Historic Anti-Chagasic Chemotherapy
    187(2)
    3 CYP51 as a Drug Target for T. cruzi Growth Inhibition
    189(2)
    4 Clinical Trials
    191(5)
    5 Evolution of Screening Cascades
    196(5)
    6 Compound Landscape for Chagas Disease Chemotherapies
    201(19)
    7 Summary
    220(11)
    References
    221(10)
    5 Imaging in Drug Development
    231(50)
    James Nairne
    Peter B. Iveson
    Andreas Meijer
    1 Introduction
    231(2)
    2 Magnetic Resonance Imaging
    233(6)
    3 Nuclear Medicine Imaging
    239(32)
    4 Summary and Future Prospects
    271(10)
    References
    272(9)
    Subject Index 281(8)
    Cumulative Index of Authors for Volumes 1--54 289(6)
    Cumulative Index of Subjects for Volumes 1--54 295
    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 tomorrows antibacterial drugs.He is a founder of INMedD, a new medicines discovery social enterprise. 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.