Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor
Date
2004-03-25ICR Author
Author
Pors, K
Paniwnyk, Z
Ruparelia, KC
Teesdale-Spittle, PH
Hartley, JA
Kelland, LR
Patterson, LH
Type
Journal Article
Metadata
Show full item recordAbstract
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 IC(50)s) against cisplatin-resistant ovarian cancer cell lines.
Collections
Language
eng
License start date
2004-03-25
Citation
JOURNAL OF MEDICINAL CHEMISTRY, 2004, 47 pp. 1856 - 1859
Publisher
AMER CHEMICAL SOC