ISSN:
1432-1335
Keywords:
2,3-Bis(2-fluoro-4-hydroxyphenyl)-2,3-dimethylbutane
;
Synthesis of their ester derivatives
;
Partial antiestrogens
;
Estrogen receptor affinity
;
Mammary-tumor-inhibiting activity
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary 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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00397917
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