1417796-40-7Relevant academic research and scientific papers
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11.(1) reversed enantioselectivity of 1,4-dioxane derivatives in α1-adrenergic and 5-HT1A receptor binding sites recognition
Bonifazi, Alessandro,Piergentili, Alessandro,Del Bello, Fabio,Farande, Yogita,Giannella, Mario,Pigini, Maria,Amantini, Consuelo,Nabissi, Massimo,Farfariello, Valerio,Santoni, Giorgio,Poggesi, Elena,Leonardi, Amedeo,Menegon, Sergio,Quaglia, Wilma
, p. 584 - 588 (2013/04/23)
5-HT1A receptor and α1-adrenoreceptor (α1-AR) binding sites recognized by the 1,4-dioxanes 2-4 display reversed stereochemical requirements. (S)-2 proved to be a potent 5-HT1A receptor agonist highly selective over α1-AR subtypes. Chirality influenced the anticancer activity of 3 and 4 in human prostate cancer cells (PC-3): (R)-4, eutomer at the α1d-AR subtype, was the most potent. The decreased effect of 4 and (R)-4 in α1d-AR silenced PC-3 cells confirmed that their anticancer activity was α1d-AR-dependent.
