E. Chao, J. Collins, S. Gaillard
Feb 15, 2006
Citations
3
Influential Citations
81
Citations
Quality indicators
Journal
Bioorganic & medicinal chemistry letters
Abstract
The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity.