Antiestrogen binding site and estrogen receptor mediate uptake and distribution of 4-hydroxytamoxifen-targeted doxorubicin-formaldehyde conjugate in breast cancer …

PJ Burke, BT Kalet, TH Koch

Index: Burke, Patrick J.; Kalet, Brian T.; Koch, Tad H. Journal of Medicinal Chemistry, 2004 , vol. 47, # 26 p. 6509 - 6518

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Citation Number: 15

Abstract

The anthracycline antitumor drug, doxorubicin (DOX), has long been used as a broad spectrum chemotherapeutic. The literature now documents the role of formaldehyde in the cytotoxic mechanism, and anthracycline-formaldehyde conjugates possess substantially enhanced activity in vitro and in vivo. We have recently reported the design, synthesis, and preliminary evaluation of a doxorubicin-formaldehyde conjugate targeted, via 4- ...