ChemInform Abstract: Indole Derivatives as a New Class of Steroid 5α-Reductase Inhibitors.
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.