744256-35-7Relevant academic research and scientific papers
Estrogen receptor ligands. Part 5: The SAR of dihydrobenzoxathiins containing modified basic side chains
Tan, Qiang,Birzin, Elizabeth T.,Chan, Wanda,Yang, Yi Tien,Pai, Lee-Yuh,Hayes, Edward C.,Dasilva, Carolyn A.,DiNinno, Frank,Rohrer, Susan P.,Schaeffer, James M.,Hammond, Milton L.
, p. 3747 - 3751 (2007/10/03)
Dihydrobenzoxathiin analogs (1-11) with modifications on the basic side chain region were prepared and evaluated for estrogen/anti-estrogen activity in both in vitro and in vivo models. The compounds generally maintained a high degree of selectivity for ERα over ERβ, similar to the original lead compound I. Many of the compounds also maintained high potency in the inhibition of human carcinoma MCF-7 cell growth. However, all were less potent in the inhibition of estradiol-triggered uterine growth. This work demonstrates the sensitive nature of modification to the antagonist basic side chain region.
