Elsevier S & T

Medicinal Chemistry of Anticancer Drugs

Avendano, Carmen; Menendez, J. Carlos

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Table of contents
  • Cover
  • Contentsv
  • Prefaceix
  • Abbreviationsxi
  • Chapter 1: Introduction1
  • 1. Some General Remarks About Cancer and Cancer Chemotherapy1
  • 2. A Brief Account of the Role of Chemistry in Cancer Chemotherapy3
  • 3. Natural Products in Cancer Chemotherapy5
  • 4. A Brief Comment About Cancer Nanotechnology6
  • 5. Conclusion7
  • References7
  • Chapter 2: Antimetabolites9
  • 1. Introduction10
  • 2. Inhibitors of the Biosynthesis of Uridylic Acid10
  • 3. Inhibitors of the Biosynthesis of 2'-Deoxyribonucleotides by Ribonucleotide Reductase (RNR)11
  • 4. Inhibitors of the Biosynthesis of Thymidilic Acid18
  • 5. Inhibitors of Dihydrofolate Reductase (DHFR)32
  • 6. Inhibitors of the De Novo Purine Biosynthesis Pathway36
  • 7. Inhibitors of Adenosine Deaminase42
  • 8. Inhibitors of Late Stages in DNA Synthesis45
  • 9. Antimetabolite Enzymes50
  • References
  • Chapter 3: Anticancer Drugs That Inhibit Hormone Action53
  • 1. Introduction54
  • 2. Estrogens and Their Involvement in Carcinogenesis54
  • 3. Antiestrogens as Antitumor Drugs58
  • 4. Aromatase Inhibitors65
  • 5. Steroid Sulfatase Inhibitors73
  • 6. Androgen-Related Antitumor Agents75
  • 7. Regulation of Steroidal Hormone Synthesis as a Target for Antitumor Drugs79
  • 8. Miscellaneous Steroid Hormone-Related Anticancer Therapy85
  • 9. Compounds Acting on Other Proteins of the Nuclear Receptor Superfamily: Retinoids86
  • References
  • Chapter 4: Anticancer Drugs Acting via Radical Species, Photosensitizers and Photodynamic Therapy of93
  • 1. Introduction: Radicals and Other Reactive Oxygen Species93
  • 2. Biological Effects of ROS95
  • 3. Anthracyclines and Their Analogs102
  • 4. Mitoxantrone and Related Quinones112
  • 5. Actinomycin D114
  • 6. Chartreusin, Elsamicin A, and Related Compounds116
  • 7. Bleomycins116
  • 8. Enediyne Antibiotics122
  • 9. Tirapazamine126
  • 10. Penclomedine128
  • 11. Radiosensitizers129
  • 12. Photodynamic Therapy of Cancer132
  • References
  • Chapter 5: DNA Alkylating Agents139
  • 1. Introduction139
  • 2. Nitrogen Mustards141
  • 3. Aziridines (Ethyleneimines)154
  • 4. Epoxides158
  • 5. Methanesulfonates159
  • 6. Nitrosoureas160
  • 7. Triazenes165
  • 8. Methylhydrazines166
  • 9. 1,3,5-Triazines: Hexamethylmelamine and Trimelamol168
  • 10. Platinum Complexes169
  • 11. Miscellaneous Alkylating and Acylating Antitumor Agents173
  • References
  • Chapter 6: Alkylating and Non-Alkylating Compounds Interacting with the DNA Minor Groove177
  • 1. Introduction177
  • 2. Netropsin, Distamycin, and Related Compounds178
  • 3. Mitomycins182
  • 4. Tetrahydroisoquinoline Alkaloids189
  • 5. Cyclopropylindole Alkylating Agents193
  • 6. Pyrrolo[1,4]Benzodiazepines195
  • References
  • Chapter 7: DNA Intercalators and Topoisomerase Inhibitors199
  • 1. DNA Intercalation and Its Consequences200
  • 2. Monofunctional Intercalating Agents201
  • 3. Bifunctional Intercalating Agents206
  • 4. DNA Topoisomerases209
  • 5. Topoisomerase II Poisons213
  • 6. Topoisomerase II Catalytic Inhibitors218
  • 7. Specific Topoisomerase I Inhibitors220
  • References
  • Chapter 8: Anticancer Drugs Targeting Tubulin and Microtubules229
  • 1. Introduction229
  • 2. Drugs That Inhibit Microtubule Polymerization at High Concentrations231
  • 3. Microtubule-Stabilizing Agents: Compounds Binding at the Taxane Site237
  • 4. Miscellaneous Anticancer Drugs Acting on Novel Sites on Tubuline245
  • 5. Antivascular Effects of Microtubule-Targeted Agents245
  • 6. Mitotic Kinesin Inhibitors246
  • References
  • Chapter 9: Drugs That Inhibit Signalling Pathways for Tumor Cell Growth and Proliferation251
  • 1. Introduction: The Role of Protein Kinases in Cancer252
  • 2. Signalling Pathways Related to Kinases254
  • 3. Inhibitors of Tyrosine Kinases (TKs)254
  • 4. Inhibitors of Serine-Threonine Kinases275
  • 5. Inhibitors of the RAS-RAF-MEK Signalling Pathway and Farnesyl Transferase286
  • 6. Inhibitors of Farnesyldiphosphate Synthase and Geranylgeranyldiphosphate Synthase295
  • 7. Anticancer Drugs Acting on Apoptotic Signalling Pathways296
  • 8. Inhibitors of Heat-Shock Proteins (HSP 90)299
  • References
  • Chapter 10: Other Approaches to Targeted Therapy307
  • 1. Proteasome Inhibitors
  • 2. Antiangiogenic Agents Unrelated to Kinase Signaling
  • 3. Epigenetic Therapy of Cancer
  • 4. Inhibitors of Other DNA-Associated Enzymes
  • 5. Therapy Directed at Other Targets
  • References
  • Chapter 11: Drug Targeting in Anticancer Chemotherapy351
  • 1. Introduction
  • 2. Prodrug-Based Anticancer Drug Targeting: Small-Molecule Prodrugs
  • 3. Polymer-Protein Conjugates
  • 4. Macromolecular Small-Drug Carrier Systems369
  • 5. Polymer-Directed Enzyme Prodrug Therapy (PDEPT)377
  • 6. Folate Receptor-Targeted Chemotherapy and Immunotherapy of Cancer378
  • 7. Liposomes and Nanoparticles in Anticancer Drug Targeting
  • References
  • Chapter 12: Drugs That Modulate Resistance to Antitumor Agents387
  • 1. ATP-Binding Cassette Efflux Pumps in Anticancer Drug Resistance388
  • 2. Glutathione and Glutathione-S-Transferase in Anticancer Drug Resistance397
  • 3. Chemosensitizers Targeting DNA-Repair Systems401
  • 4. Antitumor Drug Resistance Related to Extracellular pH: Tumor-Associated Carbonic Anhydrase as an412
  • References414
  • Chapter 13: Cancer Chemoprevention417
  • 1. Introduction417
  • 2. Ligands for Nuclear Receptors in Cancer Chemoprevention418
  • 3. Anti-Inflammatory Agents and Antioxidants in Cancer Chemoprevention421
  • 4. Chromatin Modifiers in Cancer Chemoprevention425
  • 5. Miscellaneous Agents for Chemoprevention426
  • 6. Cancer Vaccines428
  • References
  • Index431
Book details
  • Vendor Elsevier S & T
  • SKU 9780444528247
  • ISBN-13 9780080559629
  • Author Avendano, Carmen; Menendez, J. Carlos
  • Category Medical
  • Subject Pharmacology

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Antitumor chemotherapy is nowadays a very active field of research, and a huge amount of information on the topic is generated every year. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book addresses the need for an updated treatment from the point of view of medicinal chemistry and drug design. The focus of Medicinal Chemistry of Anticancer Drugs is on the mechanism of action of antitumor drugs from the molecular point of view and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents, aiming at the rationalization of the action of this type of drug, which would allow the design of new active structures.

* Explains the biological basis of cancer treatment and the role of chemists in improving anticancer drugs
* Provides the historical background and serves as a comprehensive and practical guide on cancer research and anticancer drug development
* Includes coverage of different approaches to treating cancer, drug resistance, and a chapter on cancer prevention