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