Estrogen-bridged purines: A new series of anti-tumor agents which alter cell membrane properties |
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Authors: | David Kessel W.Barkley Butler Vaidyanathan K. Iyer Jerome P. Horwitz |
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Affiliation: | 1. Department of Oncology, Wayne State University School of Medicine, Detroit, MI 48201 USA;2. Department of Pharmacology, Wayne State University School of Medicine, Detroit, MI 48201 USA;3. Michigan Cancer Foundation, Detroit, MI 48201 USA |
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Abstract: | An estrogen-bridged adenine derivative was equitoxic to both the P388 murine leukemia and an adriamycin-resistant subline, . The drug rapidly altered several P388 and membrane properties resulting in impaired nucleoside transport and increased membrane hydrophobicity. Resistance to anthracyclines in is associated with an operational barrier to drug retention which was reversed by exposure to the estrogen-bridged adenine derivative. These results suggest further exploration of the estrogen-bridged purines as chemotherapeutic agents. |
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