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N-(4-Hydroxyphenyl)-N-(1,1,1-trifluoro-2-propyl)-4-hydroxybenzamide: synthesis and pharmacological evaluation of a new antiestrogen

Hartmann, Rolf W. ; Vom Orde, Hans Dieter ; Heindl, Alexander ; Schönenberger, Helmut


4-HOC6H4N(CHMeCF3)COC6H4OH-4 (I) was prepd. by reaction of 4-MeOC6H4N:PPh3 with MeCOCF3, followed by redn., acylation with 4-MeOC6H4COCl, and demethylation. I had a relative binding affinity for the estradiol receptor of 2.4, cf. estradiol 100. It had no atitumor activity agonist hormone-dependent mammary tumors.

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