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.
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
PIERGENTILI, Alessandro;DEL BELLO, FABIO;GIANNELLA, Mario;PIGINI, Maria;AMANTINI, Consuelo;NABISSI, MASSIMO;SANTONI, Giorgio;QUAGLIA, Wilma
2013-01-01
Abstract
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.File in questo prodotto:
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