Novel 10β-thiiranyl steroids as aromatase inhibitors
Abstract
The novel 10β-thiiranyl-4-estrene-3,17-diones (5) and (6) have been synthesized by the action of triphenylphosphine sulphide–picric acid on oxirane precursors and show potent inhibition of placental aromatase; the (19R)-isomer (5) is 75 times more effective than the (19S)-isomer (6).