Synthesis of enterolactone and enterodiol precursors as potential inhibitors of human estrogen synthetase (aromatase)

A series of variably substituted derivatives of lignan lactones and diols were prepared using tandem conjugate addition reaction as a key step. These theoretical precursors of the mammalian lignans enterolactone 1 and enterodiol 3 are moderate or weak inhibitors of human aromatase activity.

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Bibliographische Detailangaben
Veröffentlicht in:	Steroids 2000-08, Vol.65 (8), p.437-441
Hauptverfasser:	Mäkelä, Taru H, Wähälä, Kristiina T, Hase, Tapio A
Format:	Artikel
Sprache:	eng
Schlagworte:	4-Butyrolactone - analogs & derivatives 4-Butyrolactone - chemical synthesis 4-Butyrolactone - chemistry 4-Butyrolactone - pharmacology Aromatase Inhibitors Catechols - chemical synthesis Catechols - pharmacology Chemistry Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Exact sciences and technology Humans Lactones Lignan Lignans - chemistry Michael reactions Noncondensed benzenic compounds Organic chemistry Phenols - chemical synthesis Phenols - pharmacology Preparations and properties Synthesis
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Beschreibung
Zusammenfassung:	A series of variably substituted derivatives of lignan lactones and diols were prepared using tandem conjugate addition reaction as a key step. These theoretical precursors of the mammalian lignans enterolactone 1 and enterodiol 3 are moderate or weak inhibitors of human aromatase activity.
ISSN:	0039-128X 1878-5867
DOI:	10.1016/S0039-128X(00)00104-5