Volume 28, Issue 16
Heterocyclic Compounds
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ChemInform Abstract: Indole Derivatives as a New Class of Steroid 5α-Reductase Inhibitors.

H. TAKAMI

H. TAKAMI

Kyowa Hakko Co., Ltd., Chiyoda, Tokyo 100, Japan

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H. KOSHIMURA

H. KOSHIMURA

Kyowa Hakko Co., Ltd., Chiyoda, Tokyo 100, Japan

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N. KISHIBAYASHI

N. KISHIBAYASHI

Kyowa Hakko Co., Ltd., Chiyoda, Tokyo 100, Japan

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A. ISHII

A. ISHII

Kyowa Hakko Co., Ltd., Chiyoda, Tokyo 100, Japan

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H. NONAKA

H. NONAKA

Kyowa Hakko Co., Ltd., Chiyoda, Tokyo 100, Japan

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S. AOYAMA

S. AOYAMA

Kyowa Hakko Co., Ltd., Chiyoda, Tokyo 100, Japan

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H. KASE

H. KASE

Kyowa Hakko Co., Ltd., Chiyoda, Tokyo 100, Japan

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T. KUMAZAWA

T. KUMAZAWA

Kyowa Hakko Co., Ltd., Chiyoda, Tokyo 100, Japan

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First published: 04 August 2010

Abstract

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ChemInform Abstract

A series of indole derivatives with varied substituents on the α, β-unsaturated double bond is synthesized and evaluated for their ability to inhibit rat prostatic 5α-reductase. The structure of the linking unit between the anilide moiety and indole skeleton is important in determining the activity. An ethyl instead of a methyl substituent results in enhanced inhibitory activity. Compound (I) shows the maximum potency with a 20-fold higher potency than the steroidal inhibitor MK-906.

chemical structure image

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