@article {Pors607, author = {Pors, Klaus and Paniwnyk, Zennia and Teesdale-Spittle, Paul and Plumb, Jane A. and Willmore, Elaine and Austin, Caroline A. and Patterson, Laurence H.}, title = {Alchemix: A Novel Alkylating Anthraquinone with Potent Activity against Anthracycline- and Cisplatin-resistant Ovarian Cancer}, volume = {2}, number = {7}, pages = {607--610}, year = {2003}, publisher = {American Association for Cancer Research}, abstract = {Chloroethylaminoanthraquinones are described with intercalating and alkylating capacity that potentially covalently cross-link topoisomerase II (topo II) to DNA. These compounds have potent cytotoxic activity (IC50 = 0.9{\textendash}7.6 nm) against the A2780 human ovarian carcinoma cell line. Hydroxyethylaminoanthraquinones also reported in this paper have similar IC50 values (0.7{\textendash}1.7 nm) in the same cell line. Alchemix (ZP281M, 1-{2-[N,N-bis(2-chloroethyl)amino]ethylamino}-4-{2-[N,N-(dimethyl)amino]ethylamino}-5,8-dihydroxy-9,10-anthracenedione), an alkylating anthraquinone, retains excellent antitumor activity in Adriamycin-resistant (2780AD) and cisplatin-resistant (2780/cp70) cell lines in vitro and in vivo. This indicates that Alchemix can evade both P-glycoprotein efflux pump and DNA mismatch repair-mediated resistance. In treated cells, Alchemix was shown to preferentially induce drug-stabilized covalent bound topo IIα-DNA complexes over topo IIβ-DNA complexes.}, issn = {1535-7163}, URL = {https://mct.aacrjournals.org/content/2/7/607}, eprint = {https://mct.aacrjournals.org/content/2/7/607.full.pdf}, journal = {Molecular Cancer Therapeutics} }