Schwarz, W. and Hartmann, R. W. and Engel, J. and Schneider, M. R. and Schönenberger, Helmut (1989) Ester derivatives of the mammary-tumor-inhibiting antiestrogen 2,3-bis(2-fluoro-4-hydroxyphenyl)-2,3-dimethylbutane. Journal of cancer research and clinical oncology 115 (2), pp. 161-165.
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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.
|Additional information (public):||GERMANY, WEST: Germany, Federal Republic of|
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Retired Professors > Prof. Schönenberger|
|Keywords:||Animals *Antineoplastic Agents Binding, Competitive Estrogen Antagonists: CS, chemical synthesis *Estrogen Antagonists: PD, pharmacology Mammary Neoplasms, Experimental: ME, metabolism Mammary Neoplasms, Experimental: PA, pathology *Mammary Neoplasms, Experimental: PC, prevention & control Mice Receptors, Estradiol: DE, drug effects 0 (Antineoplastic Agents) 0 (Estrogen Antagonists) 0 (Receptors, Estradiol)|
|Subjects:||500 Science > 540 Chemistry & allied sciences|
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Yes|
|Deposited On:||12 Nov 2010 07:26|
|Last Modified:||12 Nov 2010 07:26|