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Samenvatting Medicinale chemie deel DNA boek 1
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Schema medicinale chemie deel DNA boek 1
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By: yolo1234 • 4 months ago
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Nessie81
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DNA Rechtstreeks
o Intercalatie: vlakke structuur die past tussen opeenvolgende bp waardoor
lokaal de structuur verandert DNA niet meer herkend door enzymen
DNA vervult functie niet meer
Anthracycline antibiotica: antitumoraal (te toxisch als antibioticum),
structuur: aminoglycoside (in mineure groeve) + vlak gedeelte
Adriamycine/doxorubicine
Chinon: vrije radicalen Daunomycine/daunorubicine
cardiotoxiciteit Dactinomycine: antitumoraal (te toxisch als antibioticum)
Synthetische verbindingen
Amsacrine
Mitoxantrone
Ellipticine
o Binding en doorbraak: vorming vrije radicalen superoxideradicalen, ook
onrechtstreeks
Bacteriële + protozoa infecties (antibiotica)
Nitrofuranen en –imidazolen
o Nitrofurantoine
o Nitrofurazone NO2: activiteit
o Nifurtoinol
Imidazool/furaan: redoxpotentiaal NO2
o Metronidazol
enkel in anaerobe cellen
o Nimorazol
o Tinidazol Subtituenten: redoxpotentiaal
o Ornidazol
Antitumoraal
Anthracyclines
Bleomycine: enkel in aerobe cellen, ook onrechtstreeks, stabiele
vorm (Cu), actieve vorm (Fe)
o Alkylerend: antitumoraal
Direct
2-Haloalkylamines: vorming aziridiniumion intermediair, R-groep
draagt bij tot reactiviteit en oplosbaarheid
o Melfalan
o Estramustine (prostaatcarcinoom)
Methaansulfonaten
o Busulfam: kruisverbindingen
Ethyleenimines
o Thiotepa: 2 manieren van alkyleren
Aryltriazines: aromatische groep met 3 opeenvolgende N
o Dacarbazine: 2 manieren van alkyleren
Enzymatische activatie
Reductie: vaak een chinon
o Mitomycine C: kruisverbindingen
o Anthracyclines
o Camptothecine: kruisverbindingen
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