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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.

Front Cover; Medicinal Chemistry of Anticancer Drugs; Copyright; Contents; Foreword; Preface; Abbreviations; Chapter 1: General Aspects of Cancer Chemotherapy; 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 DrugsReferences; Chapter 2: Antimetabolites That Interfere with Nucleic Acid Biosynthesis; 1. Introduction; 2. Inhibitors of the Biosynthesis of Uridylic Acid; 3. Inhibitors of Ribonucleotide Reductase; 3.1. Structure and Catalytic Cycle of Ribonucleotide Reductase; 3.2. Gallium Salts and Complexes; 3.3. Radical Scavengers; 3.4. Substrate Analogs as Ribonucleotide Reductase Inhibitors; 3.5. Allosteric Inhibition of Ribonucleotide Reductase via Inhibition of Purine Nucleoside Phosphorylase; 4. Inhibitors of the Biosynthesis of Thymidilic Acid.

4.1. Thymidylate Synthase4.2. 5-Fluorouracil and Floxuridine; 4.3. 5-Fluorouracil Prodrugs; 4.4. Modulation of 5-Fluorouracil Activity; 4.4.1. Decreased Degradation of 5-FU; 4.4.2. Enhancement of the Inhibition of Thymidylate Synthase by 5-FU; 4.4.3. Enhancement of 5-FU Activation; 4.5. Trifluridine; 4.6. Folate-Based Thymidylate Synthase Inhibitors; 5. Inhibitors of Dihydrofolate Reductase; 5.1. Classical DHFR Inhibitors; 5.2. Nonclassical (Lipophilic) DHFR Inhibitors; 6. Inhibitors of the De Novo Purine Biosynthesis Pathway; 6.1. Inhibitors of PRPP Amidotransferase.

6.2. Inhibitors of Glycinamide Ribonucleotide Formyltransferase6.3. Inhibitors of Phosphoribosylformylglycinamidine Synthetase; 6.4. Inhibitors of 5-Aminoimidazole-4-Carboxamide Ribonucleotide Formyltransferase; 6.5. Thiopurines and Related Compounds; 7. Inhibitors of Adenosine Deaminase; 8. Inhibitors of Late Stages in DNA Synthesis; 8.1. Pyrimidine Nucleosides; 8.2. Purine Nucleosides; 9. Antimetabolite Enzymes; References; Chapter 3: Anticancer Drugs That Modulate Hormone Action; 1. Introduction; 2. Estrogens and Their Involvement in Carcinogenesis; 3. Antiestrogens as Antitumor Drugs.

3.1. Nonsteroidal Antiestrogens (Selective Estrogen Receptor Modulators)3.2. Steroidal Antiestrogens; 4. Aromatase Inhibitors; 4.1. Aromatase Mechanism of Action; 4.2. Steroidal Aromatase Inhibitors (Type I Inhibitors); 4.3. C-19 Modified Substrate Analogs; 4.4. 4-Hydroxyandrostenedione Derivatives; 4.5. Steroids with Additional Unsaturations at the A and B Rings; 4.6. Structure-Activity Relationships in Steroidal Aromatase Inhibitors; 4.7. Nonsteroidal Aromatase Inhibitors (Type II); 5. Steroid Sulfatase Inhibitors; 6. Androgen-Related Antitumor Agents; 6.1. Antiandrogens.