6,7-Dihydro-4H-indolones: synthesis and biological properties.
Syntheses of 6,7-dihydro-4H-indolones 6 and 10 by a selective Birch reduction of the benzene ring of the indole system are described. The antiestrogen zindoxifene and the 2-phenylindole 2 as well as 6 and 10 were tested for their relative binding affinities at the androgen receptor as well as for antiandrogenic and estrogenic properties. Both compounds 6 and 10 showed potent indirect antiandrogenic activity which were similar to those of the 2-phenyl-indoles zindoxifene and 2.
Schiller
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CD
Institut für Pharmazie, Lehrstuhl für Pharmazeutische Chemie II, Universität Regensburg.
von Angerer
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E
Schneider
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MR
D000726:Androgen Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D004965:Estrogen Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice
D000726:Androgen Antagonists; D004965:Estrogen Antagonists; D007211:Indoles