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


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

1989-04

AUTHORS

W. Schwarz, R. W. Hartmann, J. Engel, M. R. Schneider, H. Schönenberger

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. More... »

PAGES

161-165

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/bf00397917

DOI

http://dx.doi.org/10.1007/bf00397917

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1011847012

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/2715167


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