1621595-72-9Relevant academic research and scientific papers
Design and synthesis of nonsteroidal progesterone receptor antagonists based on C,C′-diphenylcarborane scaffold as a hydrophobic pharmacophore
Fujii, Shinya,Yamada, Ayumi,Nakano, Eiichi,Takeuchi, Yuki,Mori, Shuichi,Masuno, Hiroyuki,Kagechika, Hiroyuki
, p. 264 - 277 (2014/08/05)
The progesterone receptor (PR) plays important roles in multiple physiological processes, including female reproduction. Here, we report the synthesis of nonsteroidal PR antagonists containing a boron cluster as the hydrophobic core. We found that 1,7-diphenyl-meta-carborane was the preferred substructure among the three carborane isomers. Compound 39 was the most potent PR antagonist (IC50: 29 nM). Compound 41 also exhibited potent activity (IC50: 93 nM), and did not bind to androgen receptor, glucocorticoid receptor or mineralocorticoid receptor. These compounds may be useful for investigating potential clinical applications of PR modulators.
