DeutschesFachbuch.de : Anthracyclines Chemistry and Biology II Mode of Action, Clinical Aspects and new Drugs

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Contents
Molecular Mechanisms of Anthracycline Activity
G. L. Beretta • F. Zunino 1
Anthracycline Cadiotoxicity
P. Menna • E. Salvatorelli • L. Gianni • G. Minotti 21
Daunomycin-TFO Conjugates for Downregulation of Gene Expression
M. L. Capobianco • C. V. Catapano 45
Acid-Sensitive Prodrugs of Doxorubicin
F. Kratz 73
Doxorubicin Conjugates for Selective Delivery to Tumors
J.-C. Florent • C. Monneret 99
Anthracycline-Formaldehyde Conjugates and Their Targeted Prodrugs
T. H. Koch • B. L. Barthel • B. T. Kalet • D. L. Rudnicki • G. C. P...
Sabarubicin
F.-M. Arcamone 171
Nemorubicin
M. Broggini 191
Author Index Volumes 251-283207
Subject Index 221
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Subject Index
AN-Acetylcysteine 31
Acid-sensitive prodrugs, doxorubicin 75
- rationale 74
Aclacinomycin 173
Acosamine 175
ADEPT 100, 106
A-DOXO-HYD 80
Adriamycinone 175
Albumin 79, 94
Androgen receptor 142
Anthracycline glycosides 171
Anthracyclines 1
- activity, molecular mechanisms 1
- alkylating 149, 161
- analogs, noncardiotoxic 32
- cardiotoxicity 21
- degradation, modulators 36
- DNA damaging agents 5
- intercalating agents 4
- liposomal 32
- structures 23
Anthracyclinones 171
Antibody-directed enzyme prodrug therapy (ADEPT) 106
Antibody receptor 99
Anti-gene 45
- methodology 46
Antioxidants 30
Apoptosis 181
Aroylhydrazones 31
BBacterial-directed enzyme prodrug therapy (BDEPT) 100, 116
Bioactivation, reductive 26, 27
Bis(acetoxy)alkyl doxorubicin 108
Bis-hydroxy-p-cresol conjugates 110
Bis-ketopiperazine 31
Bombesin 100
- receptors 129
BR 96-doxorubicin immunoconjugate 76, 93
CCalicheamicin 100
Carbohydrate-lectin binding 100
Carboxylesterase 142
Carboxypeptidase doxorubicin 113
Cardiomyopathy, anthracycline-induced 24
Cardiotoxic synergism 36
Cardiotoxicity 174
- acute 22
- chronic 24
- metabolic determinants 25, 30
- pharmacokinetic determinants 24
Carvedilol 31
Cell death 11
Cellular resistance 1, 13
Cleavable complex 1
c-myc 45
- promoter, target 59
Congestive heart failure (CHF) 23
Conjugates 99
Cytochrome P 450 191
DDaunoform 149
Daunomycin 45
Daunomycin-oligonucleotide conjugates,
- synthesis 48
Daunomycin-TFOs 45
- anticancer activity 67
- transcriptional inhibition 65
- binding to double-stranded DNA 61
- sequence-specific recognition of target
- sequence 62
Daunomycinone 175, 176
Daunorubicin 22, 171
- substrates 113
Daunorubicinol (DNROL) 26
Daunosamine 22, 175
Demethoxyadriamycinone 171
Dendrimers 89
Dexrazoxane 31
5-Diacetoxypentyl Dox 102
Directed-enzyme prodrug therapies, conjugates 106
Disaccharide doxorubicin analogues 171, 173
Dithiothreitol (DTT) 79, 103, 144
DNA, anthracyclines, virtual cross-linking 145
- crosslinks 191
- glycosylation 171
- virtual crosslinks 149
DNA damage 1
- reactive oxygen species 9
- topoisomerase II poisons 6
DNA repair 191
Docetaxel (DCT) 37
Doxazolidine (Doxaz) 142, 161
- targeted 161
DOX-GA 3 100, 107
DOXO-EMCH 83, 94
Doxoform 149
Doxorubicin 1, 22, 171
Doxorubicin conjugates, albumin 78
- dendritic polymers 89
- HPMA copolymers 88
- lactosaminated albumin 84
- poly(ethylene glycol) 86
- transferrin 78
Doxorubicin immuno-conjugates 100
Doxorubicin maleimide 80
Doxorubicin prodrugs, acid-labile 73
- acid-sensitive 73
- albumin-binding 94
- antibodies 75
- clinical trials 92
- serum proteins 78
- synthetic polymers 86
Doxorubicin, targeting 99
Doxorubicin/formaldehyde prodrugs,
- co-administration 165
Doxorubicinol (DOXOL) 26
Doxsaliform 142, 155
- targeted 155
Drug conjugates 73
EEndocytosis 75
Endopeptidase legumain 124
Epidoxoform 149
Epirubicin 22, 172
Epirubicinol (EPIOL) 26, 35
Estrogen receptor 142
Ethacrynic acid 181
Extracellular THIMET oligopeptidase (TOP) 125
Extracellularly tumor activated prodrug (ETAP) 125
FFolate 100
- receptor 126
Formaldehyde, mediator of anthracycline-DNA cross-linking 141
GGastrin-releasing peptide (BN/GRP) 129
Gene-directed prodrug therapy (GDEPT) 100, 111
Glucuronide conjugates 100, 107
HHER 2 38
Hexyloxy-galactosyl-butyl doxorubicin 109
HIV 45, 57
HMPA-copolymer-ß-lactame-Dox 115
HMR 1826 100, 107
Human serum albumin, binding 180
IIdarubicin 22, 171
Idarubicinol (IDAOL) 26
Idarubicinone 176
IMMU-110 105
Integrin 100, 142
- receptor 131
Inulin multi-methacrylate (IMMA) 133
Iron chelators 31
KKaposi's sarcoma, AIDS-related 22
LLEAPT 100, 117
Lectin-directed enzyme-activated prodrug therapy (LEAPT) 117
Lectins 100
Legumain 100
Leukemia 22, 173
LHRH receptors 100
L-HSA-DOXO 84
Linkers, pH-dependent 73
Liposomal formulation 25
Luteinizing hormone releasing receptors (LHRH) 130
MMatrix metalloproteinases (MMPs) 121
Maximum tolerated dose (MTD) 183
Melatonin 31
Membrane permeable thiol-reducing agents 31
Mercaptalbumin 81
Metalloproteinase 100
Multidrug resistance (MDR) 173
Mylotarg 100
Myoglobinn 29
NNemorubicin, clinical studies 203
- cytotoxicity 198
- in vitro activity 198
- in vivo activity 200
- mechanism 201
- metabolism/pharmacokinetics 193
- pharmacokinetics 193, 197
- resistant cells 191, 199
Nitroreductase doxorubicin substrates 112
Nucleo-Particules (NPs), carbohydrate-based 133
OOligonucleotides 45
Oxidative degradation/detoxification, one-electron 29
P P glycoprotein (Pgp) 24, 173
Paclitaxel 36, 101
PDEPT 100
PEG conjugates 86, 90
PEG-coated formulation 25
Pentyl PABC-Doxaz 142
PEO-b-Pasp 90
Peptidase 100
Peptide drug delivery 133
Pharmacokinetics, DOX/DOXOL, human myocardium 28
Piperidine nitroxides 31
PK 1/PK 2 34, 114
Plasmin 119
Polyketides 172
Polymer-directed enzyme prodrug therapy (PDEPT) 114
PPT, HIV-1 as target 57
Probucol 31
Prodrugs 99
- doxorubicin 73
Prostate-specific antigen (PSA) 117
Pyrrolino-Dox 129
RReactive oxygen species 26
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