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Ester derivatives of the mammary-tumor-inhibiting antiestrogen 2,3-bis(2-fluoro-4-hydroxyphenyl)-2,3-dimethylbutane.

Abstract
The synthesis of the bisacetate (8), the bisdichloroacetate (9), the biscarbamate (10) and the bisphosphate (11) of the "partial" antiestrogen 2,3-bis(2-fluoro-4-hydroxyphenyl)-2,3-dimethylbutane (7) is described. In the case of 8-10 the introduction of ester functions slightly reduces the estrogen receptor affinity of 7. However, it was strongly diminished in 11. Compared with 7 the estrogenic potency of 8-11 is moderately increased. Compounds 8-11 cause a strong inhibition of the hormone-dependent MXT M3.2 mouse mammary tumor. Only 9 containing cytotoxic dichloroacetate groups shows a significantly better antitumor effect than 7.
AuthorsW Schwarz, R W Hartmann, J Engel, M R Schneider, H Schönenberger
JournalJournal of cancer research and clinical oncology (J Cancer Res Clin Oncol) Vol. 115 Issue 2 Pg. 161-5 ( 1989) ISSN: 0171-5216 [Print] Germany
PMID2715167 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Estrogen Antagonists
  • Receptors, Estradiol
Topics
  • Animals
  • Antineoplastic Agents
  • Binding, Competitive
  • Estrogen Antagonists (chemical synthesis, pharmacology)
  • Mammary Neoplasms, Experimental (metabolism, pathology, prevention & control)
  • Mice
  • Receptors, Estradiol (drug effects)

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