Download MendeleyBenzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold.
Richardson, T.I., Norman, B.H., Lugar, C.W., Jones, S.A., Wang, Y., Durbin, J.D., Krishnan, V., Dodge, J.A.(2007) Bioorg Med Chem Lett 17: 3570-3574
- PubMed: 17485205
- DOI: https://doi.org/10.1016/j.bmcl.2007.04.051
- Primary Citation of Related Structures:
2POG - PubMed Abstract:
Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here we describe structure-activity relationship studies that led to the discovery of bezopyran 5b. X-ray crystal structures of 5b and a non-selective analog 5c in ERalpha help explain the observed selectivity of the benzopyran platform.
Organizational Affiliation:
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. t_richardson@lilly.com
