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

✍ Scribed by Claus-D. Schiller; Erwin Von Angerer; Martin R. Schneider

Book ID
101642616
Publisher
John Wiley and Sons
Year
2010
Tongue
English
Weight
361 KB
Volume
324
Category
Article
ISSN
0365-6233

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✦ Synopsis

Abstract

Syntheses of 6,7‐dihydro‐4__H__‐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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