Structure-Activity Relationship of

Autor: David, Sedlák, Tyler A, Wilson, Werner, Tjarks, Hanna S, Radomska, Hongyan, Wang, Jayaprakash Narayana, Kolla, Zbigniew J, Leśnikowski, Alena, Špičáková, Tehane, Ali, Keisuke, Ishita, Liva Harinantenaina, Rakotondraibe, Sandip, Vibhute, Dasheng, Wang, Pavel, Anzenbacher, Chad, Bennett, Petr, Bartunek, Christopher C, Coss
Rok vydání: 2021
Předmět:
Zdroj: Journal of medicinal chemistry. 64(13)
ISSN: 1520-4804
Popis: Selective agonism of the estrogen receptor (ER) subtypes, ERα and ERβ, has historically been difficult to achieve due to the high degree of ligand-binding domain structural similarity. Multiple efforts have focused on the use of classical organic scaffolds to model 17β-estradiol geometry in the design of ERβ selective agonists, with several proceeding to various stages of clinical development. Carborane scaffolds offer many unique advantages including the potential for novel ligand/receptor interactions but remain relatively unexplored. We synthesized a series of
Databáze: OpenAIRE