Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold.
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Richardson TI, Norman BH, Lugar CW, Jones SA, Wang Y, Durbin JD, Krishnan V, Dodge JA
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 2: structure-activity relationship studies on the benzopyran scaffold.
Bioorg Med Chem Lett. 2007 Jul 1;17(13):3570-4. Epub 2007 Apr 25.
- PubMed ID
- 17485205 [ View in 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) (3AS,4R,9BR)-4-(4-HYDROXYPHENYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-9-OL Estrogen receptor alpha Ki (nM) 0.35 7.5 22 Details Erteberel Estrogen receptor alpha Ki (nM) 4.34 7.5 22 Details Erteberel Estrogen receptor beta Ki (nM) 0.47 7.5 22 Details