Abstract
The synthesis of eight 16α-propyl derivatives of estradiol is described, and structure-activity relationships are discussed. Potent inhibitors of cytosolic 17β-hydroxysteroid dehydrogenase of human placenta (type 1) can be obtained when a good leaving group is located at the end of a 16α-propyl side chain; the 16α-(iodopropyl)-estradiol ( 7) and 16α-(bromopropyl)-estradiol ( 6) gave the best irreversible inhibitions of 17β-HSD type 1, with IC 50 values of 0.42 and 0.46 μM, respectively.
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