Medicinal Chemistry of Anticancer Drugs

Medicinal Chemistry of Anticancer Drugs

2nd Edition - April 28, 2015

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  • Authors: Carmen Avendano, J. Carlos Menendez
  • Paperback ISBN: 9780444626493
  • eBook ISBN: 9780444626677

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Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design.

Key Features

  • Presents information in a clear and concise way using a large number of figures
  • Historical background provides insights on how the process of drug discovery in the anticancer field has evolved
  • Extensive references to primary literature


For researchers in pharmaceutical, medicinal and organic chemistry departments in both academia and industry. Practitioners requiring an understanding of structure-activity relationships in oncology / cancer research. Advanced undergraduate and graduate students in medicinal chemistry and pharmacology.

Table of Contents

    • Foreword
    • Preface
    • Abbreviations
    • Chapter 1: General Aspects of Cancer Chemotherapy
      • Abstract
      • 1. Introduction: Some General Comments About Cancer
      • 2 Tumorigenesis and Oncogenes: Pharmacogenomics
      • 3 Early Diagnosis of Cancer and Its Therapeutic Relevance
      • 4 A Brief History of Cancer Chemotherapy
      • 5 General Comments About Anticancer Drug Discovery
      • 6 Combination Therapy and Personalized Anticancer Treatments
      • 7 Natural Products in Cancer Chemotherapy
      • 8 A Brief Comment About Cancer Nanotechnology
      • 9 Summary of FDA-Approved Anticancer Drugs
    • Chapter 2: Antimetabolites That Interfere with Nucleic Acid Biosynthesis
      • Abstract
      • 1 Introduction
      • 2 Inhibitors of the Biosynthesis of Uridylic Acid
      • 3 Inhibitors of Ribonucleotide Reductase
      • 4 Inhibitors of the Biosynthesis of Thymidilic Acid
      • 5 Inhibitors of Dihydrofolate Reductase
      • 6 Inhibitors of the De Novo Purine Biosynthesis Pathway
      • 7 Inhibitors of Adenosine Deaminase
      • 8 Inhibitors of Late Stages in DNA Synthesis
      • 9 Antimetabolite Enzymes
    • Chapter 3: Anticancer Drugs That Modulate Hormone Action
      • Abstract
      • 1 Introduction
      • 2 Estrogens and Their Involvement in Carcinogenesis
      • 3 Antiestrogens as Antitumor Drugs
      • 4 Aromatase Inhibitors
      • 5 Steroid Sulfatase Inhibitors
      • 6 Androgen-Related Antitumor Agents
      • 7 Regulation of Gonadotropin-Releasing Hormone: Control of the Hypothalamic–Pituitary–Gonadal axis
      • 8 Miscellaneous Steroid Hormone-Related Anticancer Therapy
      • 9 Compounds Acting on Other Proteins of the Nuclear Receptor Superfamily: Retinoids
      • 10 PPAR Ligands as Antitumor Agents
      • 11 Somatostatin Analogs in Neuroendocrine Tumors
    • Chapter 4: Anticancer Drugs Acting via Radical Species: Radiotherapy and Photodynamic Therapy of Cancer
      • Abstract
      • 1 Introduction: Radicals and Other Reactive Oxygen Species
      • 2 Biological Effects of Reactive Oxygen Species
      • 3 Anthracyclines and Their Analogs
      • 4 Mitoxantrone and Related Quinones
      • 5 Actinomycin D
      • 6 Chartreusin, Elsamicin A, and Related Compounds
      • 7 Bleomycins
      • 8 Enediyne Antibiotics
      • 9 Tirapazamine
      • 10 Penclomedine
      • 11 Radiotherapy and Radiosensitizers
      • 12 Photodynamic Therapy of Cancer
    • Chapter 5: DNA Alkylating Agents
      • Abstract
      • 1 Introduction
      • 2 Nitrogen Mustards
      • 3 Aziridines (Ethyleneimines)
      • 4 Epoxides
      • 5 Methanesulfonates
      • 6 Nitrosoureas
      • 7 Triazenes
      • 8 Methylhydrazines
      • 9 1,3,5-Triazines: Hexamethylmelamine and Trimelamol
      • 10 Transition Metal Species
      • 11 Miscellaneous Alkylating and Acylating Antitumor Agents
    • Chapter 6: Anticancer Drugs That Interact with the DNA Minor Groove
      • Abstract
      • 1 Introduction
      • 2 Netropsin, Distamycin, and Related Compounds
      • 3 Mitomycins
      • 4 Tetrahydroisoquinoline Alkaloids
      • 5 Cyclopropylindole Alkylating Agents
      • 6 Irofulven
      • 7 Pyrrolo[1,4]benzodiazepines
    • Chapter 7: Other Anticancer Drugs Targeting DNA and DNA-Associated Enzymes
      • Abstract
      • 1 DNA Intercalation and Its Consequences
      • 2 Monofunctional Intercalating Agents
      • 3 Bifunctional Intercalating Agents
      • 4 Indirect DNA Damage by DNA Topoisomerase Inhibitors
      • 5 Specific Topoisomerase I Inhibitors
      • 6 Topoisomerase II Poisons
      • 7 Topoisomerase II Catalytic Inhibitors
      • 8 Telomerase Inhibitors and Other Anticancer Approaches Targeting TelomerEs
      • 9 DNA Repair Inhibitors
    • Chapter 8: Epigenetic Therapy of Cancer
      • Abstract
      • 1 Introduction
      • 2 Inhibitors of DNA Methylation: Reactivation of Silenced Genes
      • 3 Inhibitors of Histone and Other Protein Deacetylases
      • 4 Regulators of Histone Methylation
    • Chapter 9: Anticancer Drugs Targeting Tubulin and Microtubules
      • Abstract
      • 1 Introduction
      • 2 Drugs That Inhibit Microtubule Polymerization
      • 3 Microtubule-Stabilizing Agents: Compounds Binding at the Taxane Site
      • 4 Miscellaneous Anticancer Drugs Acting on Novel Sites of Tubuline
      • 5 Antivascular Effects of Microtubule-Targeted Agents
      • 6 Mitotic Kinesin Inhibitors
    • Chapter 10: Drugs That Inhibit Signaling Pathways for Tumor Cell Growth and Proliferation: Kinase Inhibitors
      • Abstract
      • 1 Introduction
      • 2 Oncogenes and Signal Transduction
      • 3 The Role of Protein Kinases in Cancer: Signaling Pathways Related to Kinases
      • 4 Inhibitors of Tyrosine Kinases
      • 5 Inhibitors of Serine–Threonine Kinases
      • 6 Inhibitors of the Ras/Raf/MEK Signaling Pathway
      • 7 Transforming Growth Factor-β–Smad Signaling
      • 8 Glucose Metabolism and Cancer: Inhibitors of Kinases Involved in Anaerobic Glycolysis
    • Chapter 11: Other Nonbiological Approaches to Targeted Cancer Chemotherapy
      • Abstract
      • 1 Introduction
      • 2 Proteolytic Enzymes as Anticancer Targets
      • 3 Heparanase Inhibitors
      • 4 Integrin Antagonists and Inhibitors of Chemokine Receptors
      • 5 Endogenous Inhibitors of Angiogenesis
      • 6 Miscellaneous Antiangiogenic Compounds
      • 7 Drugs Targeting Cancer Stem Cells
      • 8 Inhibitors of Oncogenic Protein–Protein Interactions
      • 9 Anticancer Agents Targeted at the Lysosomes
    • Chapter 12: Biological Therapy of Cancer
      • Abstract
      • 1 Introduction
      • 2 Monoclonal Antibodies against Cancer Cells
      • 3 Cancer Immunotherapy: General Aspects
      • 4 Cancer Vaccines
      • 5 Gene Therapy
      • 6 Antisense Oligonucleotides in Cancer Treatment
      • 7 Bacteria and Bacterial Toxins in Cancer Therapy
    • Chapter 13: Drug Targeting in Anticancer Chemotherapy
      • Abstract
      • 1 Introduction
      • 2 Small-Molecule Prodrugs for Anticancer Drug Targeting
      • 3 Therapeutic Nanoparticles for Drug Delivery in Cancer: General Aspects
      • 4 Polymer Conjugates: Macromolecular Small-Drug Carrier Systems
      • 5 Polymer-Directed Enzyme Prodrug Therapy Approaches
      • 6 Folate Receptor-Targeted Chemotherapy
      • 7 Liposomes and Other Nanoparticles in Anticancer Drug Targeting
    • Chapter 14: Drugs That Modulate Resistance to Antitumor Agents
      • Abstract
      • 1 Introduction
      • 2 ABC Efflux Pumps in Anticancer Drug Resistance
      • 3 Glutathione and Glutathione S-Transferase in Anticancer Drug Resistance
      • 4 Chemosensitizers Targeting DNA Repair Systems
      • 5 Antitumor Drug Resistance Related to Cellular Adhesion Molecules
      • 6 Antitumor Drug Resistance Related to the Extracellular pH: Tumor-Associated Carbonic Anhydrase as an Anticancer Target
      • 7 The Role of the SPARC Protein in Drug Resistance
      • 8 Radioresistance and Tumor Radiosensitization
      • 9 Induced Tumor Chemoresistance
    • Chapter 15: Cancer Chemoprevention
      • Abstract
      • 1 Introduction
      • 2 Cancer Biomarkers, Molecular Medicine, and Individualized Treatments
      • 3 Cancer Chemoprevention
      • 4 Chemopreventive Agents
      • 5 Nutritional Supplements
      • 6 Ligands for Nuclear Receptors in Cancer Chemoprevention
    • Index

Product details

  • No. of pages: 768
  • Language: English
  • Copyright: © Elsevier Science 2015
  • Published: April 28, 2015
  • Imprint: Elsevier Science
  • Paperback ISBN: 9780444626493
  • eBook ISBN: 9780444626677

About the Authors

Carmen Avendano

Carmen Avendano
Mª del Carmen Avendaño López received her doctoral degree in Pharmacy at the Complutense University of Madrid (UCM) in 1970. In 1986, she became Full Professor of Organic Chemistry at the Department of Organic and Pharmaceutical Chemistry of this university, being responsible for one of its research groups. Between 1993 and 2009, she was a member of the Scientific Advising Committee for the Profarma Program, organized by the Spanish Ministry for Industry to incentivize research activities at the pharmaceutical industry. She was appointed Vice-rector in charge of Postgraduate Degrees at the International University “Menéndez y Pelayo” in 2005-2007. She participated in the development of the Spanish Society for Therapeutical Chemistry and has also been a member of several scientific international societies and assessment committees. Since 1999, she is a Fellow of the Spanish National Royal Academy of Pharmacy where she is in charge of all activities related to Medicinal Chemistry, with particular focus on the relevance of chemistry in drug discovery and development. She has co-authored several chapters in periodical series and encyclopedias, including “Comprehensive Heterocyclic Chemistry” and “Science of Synthesis”, and has edited and co-authored several Medicinal Chemistry textbooks, most notably “Introducción a la Química Farmacéutica”, published by McGraw-Hill Interamericana in 1993 and 2001. In 2008, she co-authored with Dr. Menéndez the first edition of “Medicinal Chemistry of Anticancer Drugs“ for Elsevier. Her research activities, documented in about 200 publications and some patents in collaboration with the pharmaceutical industry, have dealt with the development of synthetic methodologies to obtain biologically active molecules, with particular focus on antitumor natural compounds.

Affiliations and Expertise

Full Professor, Department of Organic Chemistry, Farmaceutica, Facultad de Farmacia, Madrid, Spain

J. Carlos Menendez

J. Carlos Menendez
José Carlos Menéndez was born in Madrid (1960) and obtained degrees in Pharmacy from Universidad Complutense at Madrid, UCM (1982, with Excellence Award) and Chemistry from UNED (1985) followed by a Ph.D. in Pharmacy from UCM in 1988, under the supervision of Dr. Mónica M. Söllhuber, with Excellence Award. In August 1988, he joined the group of Professor Steven V. Ley at Imperial College, London, where he worked on the total synthesis of the natural ionophoric antibiotic routiennocin. In September 1989, he returned as a Profesor Titular to the Organic and Medicinal Chemistry Department at UCM, where he has pursued his teaching and research career ever since, having obtained Accreditation as a Full Professor in 2010. He has varied research interests, related, on one hand, to medicinal chemistry work in the fields of neurodegeneration (prion disease, Alzheimer’s disease, ischemic injury) and chemotherapy (cancer, tuberculosis, leishmaniasis). Other projects pursued in his group are focused on the development of new synthetic methodology, including work on microwave-assisted organic synthesis, CAN as a catalyst for organic synthesis, green chemistry and the development new domino and multicomponent reactions for the preparation of biologically relevant bicyclic systems and nitrogen heterocycles. This work has been documented in about 210 research papers, reviews and chapters and 9 patents. Additionally, he has co-authored two textbooks in Medicinal Chemistry for McGraw-Hill Interamericana (?Introducción a la Química Farmacéutica, 2nd Ed." 2001 and "Ejercicios de Química Farmacéutica", 1997), and a third one for Elsevier ("Medicinal Chemistry of Anticancer Drugs", 2008). He is the coordinator of a Master Course on Drug Discovery, and the coordinator at UCM of a Ph.D. program in Medicinal Chemistry. He has collaborated with many research groups in UK, Italy, France, and India and also has some long-standing collaborations with several chemical and pharmaceutical Spanish companies. He has been the head of the Organic Microanalysis service at UCM since its creation in 1991. Since 2004, he is a Corresponding Member of the Spanish Royal Academy of Pharmacy. He has been a Visiting Professor at Université Paul Cézanne (Aix-Marseille III, France) in 2007 and at the Istituto di Studi Avanzati (ISA), Bologna University, Italy, in 2014.

Affiliations and Expertise

Profesor Titular, Department of Organic Chemistry, Farmaceutica, Facultad de Farmacia, Madrid, Spain

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