No / Novel 1- and 1,4-substituted chloroethylaminoanthraquinones with DNA binding and alkylating properties along with their respective hydroxyethylaminoanthraquinone intermediates were synthesized. Selected chloroethylaminoanthraquinones were shown to cross-link DNA and alkylate guanines (at low nM concentration) with a preference for reaction sites containing 5'-PyG. A compound (Alchemix) with the bis-chloroethyl functionality confined to one side chain alkylated but did not cross-link DNA. All the 1,4-disubstituted chloroethylaminoanthraquinones were potently cytotoxic (nM IC50s) against cisplatin-resistant ovarian cancer cell lines.
Identifer | oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/3164 |
Date | January 2004 |
Creators | Pors, Klaus, Paniwnyk, Z., Patterson, Laurence H., Ruparelia, K.C., Hartley, J.A., Kelland, L.R. |
Source Sets | Bradford Scholars |
Language | English |
Detected Language | English |
Type | Article, No full-text in the repository |
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