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- W2007663268 abstract "In vivo effectiveness of doxorubicin remains restricted due to toxicity and drug resistance. Hydroxyrubicin is a synthetic analog of doxorubicin in which the basic amino group at the C-3′ has been replaced by a hydroxyl group in order to overcome recognition by the multidrug resistant (MDR) P-ghlcoprotein and limit cardiotoxicity. The present study shows that hydroxyribicin is a less potent intercalator than doxorubicin. Induction of topoisomerase II-mediated DNA cleavage in the human C-myc origin by the two drugs was similar, reaching a maximum at 0.5 μM. Results from the NCI Cell Screening program indicate a relatively good correlation between the cytotoxicity of the 2 drugs on 55 cell lines of various origins (r = 0.723). Using a donogenic assay, we observed that hydroxyrubicin was 20-fold more cytotoxic against the MDR KB-VI cell line than doxorubicin and was slightly more cytotoxic than doxorubicin in the sensitive KB3.1 cell line. Uptake studies showed that doxorubicin was retained up to I hr in KB3.1 cells and rapidly eliminated from resistant KB-VI cells. In contrast, hydroxyrubicin was rapidly eliminated from both sensitive KB3.1 and MDR-positive KB-VI cells. Both drugs induced protein-linked DNA single-strand breaks (SSBs) in both KB3.I and KB-VI cells, which is consistent with topoisomerase inhibition. However, the kinetics of DNA SSBs induced by both drugs was very different. DNA breaks disappeared quickly in both KB3.1 and KB-VI cell lines after hydroxyrubicin removal while DNA breaks induced by doxorubicin disappeared very slowly in KB3.1 cells and rapidly in KB-VI cells. We conclude that removal of the basic amino group at the C-3′ of doxorubicin modifies drug transport and partially circumvents MDR without changing topoisomerase II inhibition when compared with doxorubicin. © 1994 Wiley-Liss, Inc." @default.
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- W2007663268 title "Hydroxyrubicin, a deaminated derivative of doxorubicin, inhibits mammalian DNA topoisomerase II and partially circumvents multidrug resistance" @default.
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- W2007663268 doi "https://doi.org/10.1002/ijc.2910580115" @default.
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