Table of Contents
Preface ix
Introduction xi
1 Alkylating Agents 1
1.1 bis-Chloroethyl Amines 1
1.2 Several Other Chloroethyl Agents 5
1.3 Platinum-Based Antineoplastic Agents 6
1.4 Miscellaneous Alkylating Agents 8
2 Antimetabolites 13
2.1 Introduction 13
2.2 Folate Antagonists 14
2.3 Pyrimidines and Purines 21
3 Hormone Blocking Anticancer Drugs 31
3.1 Introduction 31
3.2 Estrogen Antagonists 32
3.3 Androgen Antagonists 44
4 Topoisomerase Inhibitors 55
4.1 Introduction 55
4.2 Anthracyclines 56
4.3 Anthraquinones and Anthrapyrazoles 59
4.4 Camptothecins 65
4.5 Miscellaneous Topoisomerase Inhibitors 74
5 Mitotic Inhibitors 81
5.1 Introduction 81
5.2 Taxanes 82
5.3 Wholly Synthetic Compounds 86
6 Matrix Metalloproteinase Inhibitors 97
6.1 Introduction 97
6.2 Hydroxamates 98
7 Histone Deacetylase Inhibitors 109
7.1 Introduction 109
7.2 Hydroxamates 110
7.3 Phenylenediamines 113
8 Enzyme Inhibitor, Part I, Tyrosine Kinases 117
8.1 Introduction 117
8.2 Epidermal Growth Factor Inhibitors 118
8.3 VEGF 124
8.4 SRC Nonreceptor Tyrosine Kinase 134
8.5 PDGF 138
8.6 EGF 141
8.7 Other TKI 143
8.8 Janus Kinase Inhibitors 154
9 Enzyme Inhibitors: Part II Additional Targets 161
9.1 Serine–Threonine Kinase Inhibitors 161
9.2 Additional Enzyme Inhibitors 166
10 Miscellaneous Antineoplastic Agents 187
10.1 Acyclic 187
10.2 Monocyclic 188
10.3 Two Linked Rings 190
10.4 Rings on a Chain 191
10.5 Fused Rings 195
Appendix A 203
Combinatorial Chemistry 203
Index of Heterocyclic Sytheses 205
Subject Index 207