Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cells
Paniwnyk, Z. Patterson, Laurence H. Ruparelia, K.C. Hartley, J.A. Kelland, L.R.
Paniwnyk, Z.
Patterson, Laurence H.
Ruparelia, K.C.
Hartley, J.A.
Kelland, L.R.
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2004
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Abstract
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.
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Pors,K., Paniwnyk, Z., Ruparelia, K.C., Teesdale-Spittle, P.H., Hartley, J.A., Kelland, L.R. and Patterson, L.H. (2004). Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cells. Journal of Medicinal Chemistry. Vol. 47, No. 7, pp. 1856-1859.
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