Anticancer Drugs That Inhibit Hormone Action

Contents 1. Introduction 54

2. Estrogens and Their Involvement in Carcinogenesis 54

3. Antiestrogens as Antitumor Drugs 58

3.1. Nonsteroidal antiestrogens (SERMs) 58

3.2. Steroidal antiestrogens 62

4. Aromatase Inhibitors 65

4.1. Aromatase mechanism of action 67

4.2. Steroidal aromatase inhibitors (type I inhibitors) 68

4.3. Nonsteroidal aromatase inhibitors (type II) 72

5. Steroid Sulfatase Inhibitors 73

6. Androgen-Related Antitumor Agents 75

6.1. Antiandrogens 76

6.2. Inhibitors of 14a-demethylase and 17a-hydroxylase 77

6.3. Inhibitors of 5a-reductase 77

7. Regulation of Steroidal Hormone Synthesis as a Target for Antitumor Drugs 79

7.1. Introduction 79

7.2. GnRH (LHRH) agonists 81

7.3. GnRH (LHRH) antagonists 82

8. Miscellaneous Steroid Hormone-Related Anticancer Therapy 85

8.1. Gestagens as antitumor agents 85

8.2. Glucocorticoids and inhibitors of their biosynthesis as antitumor agents 85

9. Compounds Acting on Other Proteins of the Nuclear Receptor Superfamily: Retinoids 86

References 90

Medicinal Chemistry of Anticancer Drugs © 2008 Elsevier B. V.

DOI: 10.1016/B978-0-444-52824-7.00003-2 All rights reserved.

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