Article
Linker length in podophyllotoxin-acridine conjugates determines potency in vivo and in vitro as well as specificity against MDR cell lines.
Anti-cancer drug design - 1 Dec 2001
Rothenborg-Jensen L, Hansen H F, Wessel I, Nitiss J L, Schmidt G, Jensen P B, Sehested M, Jensen L H
Abstract excerpt
We have synthesized two podophyllotoxin-acridine conjugates-pACR6 and pACR8. In these compounds an 9-acridinyl moiety is beta linked to the C4 carbon of the four ring system in 4'-demethylepipodophyllotoxin (epiDPT) via eighter an N-6-aminohexanylamide linker (pACR6) or via an N-8-aminooctanylamide linker containing two more carbon atoms (pACR8). The acridine-linker moiety occupies the position where different...
Topics
- Aclarubicin
- Acridines
- Antibiotics, Antineoplastic
- Antineoplastic Agents
- Biological Transport, Active
- Cell Survival
- Cross-Linking Reagents
- DNA
- DNA Damage
- DNA Topoisomerases, Type II
- Down-Regulation
- Drug Resistance, Multiple
- Drug Resistance, Neoplasm