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A novel series of indolebutyric acids with varying benzoyl substituents were synthesized to develop nonsteroidal inhibitors of steroid 5 alpha-reductase. We previously reported the discovery of a novel nonsteroidal 5 alpha-reductase inhibitor, FR119680, which had an IC50 value of 5.0 nM against the rat prostatic enzyme. However, this compound was not strongly active against the human prostatic enzyme. By further study of the structure-activity relationships we succeeded in producing the strongly active compound, FK143, 4-[3-[3-[bis(4-isobutylphenyl)-methylamino]benzoyl]-1H-indol-1-yl] butyric acid, with an IC50 value of 1.9 nM against the human enzyme. FK143 also has in vivo inhibitory activity against the castrated young rat model and it should therefore be an extremely useful agent for the treatment of benign prostatic hyperplasia.

Citation

K Sawada, S Okada, P Golden, N Kayakiri, Y Sawada, M Hashimoto, H Tanaka. 4-(1-benzoylindol-3-yl)butyric acids and FK143: novel nonsteroidal inhibitors of steroid 5 alpha-reductase (II). Chemical & pharmaceutical bulletin. 1999 Apr;47(4):481-91

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PMID: 10319427

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