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.