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6,7-Dihydro-4H-indolones: synthesis and biological properties

Schiller, C. D. ; Angerer, E. von ; Schneider, M. R.


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.

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