DNA Intercalators and Topoisomerase Inhibitors

Contents 1. DNA Intercalation and Its Consequences 200

2. Monofunctional Intercalating Agents 201

2.1. Ellipticine and its analogues 201

2.2. Actinomycins 204

2.3. Fused quinoline compounds 204

2.4. Naphthalimides and related compounds 205

2.5. Chartreusin, elsamicin A, and related compounds 206

3. Bifunctional Intercalating Agents 206

4. DNA Topoisomerases 206

4.1. Topoisomerase I mechanism 209

4.2. Topoisomerase II mechanism 209

5. Topoisomerase II Poisons 211

5.1. Acridine derivatives 213

5.2. Anthracyclines and related compounds 213

5.3. Non-intercalating topoisomerase II poisons 214

6. Topoisomerase II Catalytic Inhibitors 216

6.1. Inhibitors of the binding of topoisomerase II to

DNA: Aclarubicin 218

6.2. Merbarone 219

6.3. Bis(dioxopiperazines) 219

7. Specific Topoisomerase I Inhibitors 219

7.1. Camptothecins 220

7.2. Non-CPT topoisomerase I inhibitors 221 References 225

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

DOI: 10.1016/B978-0-444-52824-7.00007-X All rights reserved.

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