e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521
Pyrazolo [1, 5-a] pyrimidines as estrogen receptor ligands: defining the orientation of a novel heterocyclic core
…, KE Carlson, JA Katzenellenbogen
Index: Compton, Dennis R.; Carlson, Kathryn E.; Katzenellenbogen, John A. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 22 p. 5681 - 5684
We have examined the pyrazolo [1, 5-a] pyrimidine scaffold as a novel core structure for estrogen receptor ligands. Attachment of various substituents has helped to define the orientation of this heterocycle in the ligand-binding pocket as one in which a pendant phenol rather than the hydroxylpyrimidine serves as a mimic of the A-ring of estradiol.
