Synthesis and evaluation of 10β-substituted 4-estrene-3,17-diones as inhibitors of human placental microsomal aromatase

Article abstract of DOI:10.1016/0039-128X(82)90151-9

This paper describes the synthesis of a series of new 10β-substituted 4-estrene-3,17-dione analogs. These compounds, together with a number of known analogs, have been evaluated as reversible or irreversible inhibitors of human placental microsomal aromatase. The best reversible inhibitor is the 10β-vinyl compound. The only compounds causing irreversible inhibition of aromatase are the 10β-propargyl compound and the 10β-difluoromethyl compound.