A series of thiol androgens were synthesized and investigated to characterize structural features important for the inhibition of aromatase. Analogues of androstenedione with thiol groups in either the 2a-, lop-, or 19-positions caused time-dependent inhibition of human placental aromatase. When their KI and k,,, values were compared with those of 4- hydroxyandrost-4-ene-3, 17-dione (4-OHa) and 10/3-propargylestr-4-ene-3, 17-dione ( ...
