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  • Title: Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.
    Author: Richardson TI, Dodge JA, Wang Y, Durbin JD, Krishnan V, Norman BH.
    Journal: Bioorg Med Chem Lett; 2007 Oct 15; 17(20):5563-6. PubMed ID: 17804226.
    Abstract:
    Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe the synthesis of a late stage intermediate that allowed us to combine A-ring and C-ring modifications and carry out simultaneous SAR studies at both positions. Modification of both positions proved additive, maintaining affinity and improving ERbeta selectivity up to 83-fold. An X-ray cocrystal structure confirms the previously observed binding mode in ERbeta.
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