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Bioorg Med Chem Lett ; 19(4): 1250-3, 2009 Feb 15.
Article in English | MEDLINE | ID: mdl-19167882

ABSTRACT

Estradiol and related estrogens have been widely used as supplements to relieve menopausal symptoms, but they lead to an increased risk of breast and endometrial cancer. Here we report the synthesis of a new family of compounds where we have removed the B-ring from the steroid ABCD structure, and functionalized the A-ring. These A-CD compounds show a preferential affinity for the estrogen receptor subtype ERbeta. Some show binding affinities which are greater than estradiol. The presence of electron-withdrawing substituents on the A-ring should reduce the tendency of these compounds to form carcinogenic metabolites, so they might lead to a safer approach to hormone replacement therapy.


Subject(s)
Estradiol , Receptors, Estradiol/agonists , Estradiol/agonists , Estradiol/analogs & derivatives , Estradiol/chemical synthesis , Estradiol/pharmacology , Female , Hormone Replacement Therapy/methods , Humans , Models, Molecular , Molecular Structure , Structure-Activity Relationship
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