Hydroxylation at C-3′ of doxorubicin alters the selected phenotype of cellular drug resistance

Bioorganic & Medicinal Chemistry Letters
1995.0

Abstract

Hydroxylation at C-3' of doxorubicin (DOX) yields the uncharged congener hydroxyrubicin, which circumvents P-glycoprotein-mediated drug resistance without loss of topoisomerase II inhibitory activity. Hydroxyrubicin-resistant cells exhibit a phenotype that is uniquely different from DOX resistance by expressing non-functional P-glycoprotein and hypersensitivity to anti-mitotic drugs.

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