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.
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Authors | W Schwarz, R W Hartmann, J Engel, M R Schneider, H Schönenberger |
Journal | Journal of cancer research and clinical oncology
(J Cancer Res Clin Oncol)
Vol. 115
Issue 2
Pg. 161-5
( 1989)
ISSN: 0171-5216 [Print] Germany |
PMID | 2715167
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Antineoplastic Agents
- Estrogen Antagonists
- Receptors, Estradiol
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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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