Structure-Activity Relationships in 1,4-Benzodioxan-Related Compounds. 11.(1) Reversed Enantioselectivity of 1,4-Dioxane Derivatives in alpha(1)-Adrenergic and 5-HT1A Receptor Binding Sites Recognition

[摘要]：5-HT1A receptor and alpha(1)-adrenoreceptor (alpha(1)-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 alpha(1)-AR subtypes. Chirality influenced the anticancer activity of 3 and 4 in human prostate cancer cells (PC-3): (R)-4, eutomer at the alpha(1d)-AR subtype, was the most potent. The decreased effect of 4 and (R)-4 in alpha(1d)-AR silenced PC-3 cells confirmed that their anticancer activity was alpha(1d)-AR-dependent.

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