2. Academic Validation
  3. 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

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

  • J Med Chem. 2013 Jan 24;56(2):584-8. doi: 10.1021/jm301525w.
Alessandro Bonifazi 1,  Alessandro Piergentili,  Fabio Del Bello,  Yogita Farande,  Mario Giannella,  Maria Pigini,  Consuelo Amantini,  Massimo Nabissi,  Valerio Farfariello,  Giorgio Santoni,  Elena Poggesi,  Amedeo Leonardi,  Sergio Menegon,  Wilma Quaglia
Affiliations

Affiliation

  • 1 Medicinal Chemistry Unit, School of Pharmacy, University of Camerino , Via S. Agostino 1, 62032 Camerino, Italy.
PMID: 23252794 DOI: 10.1021/jm301525w
Abstract

5-HT(1A) receptor and α(1)-adrenoreceptor (α(1)-AR) binding sites recognized by the 1,4-dioxanes 2-4 display reversed stereochemical requirements. (S)-2 proved to be a potent 5-HT(1A) receptor agonist highly selective over α(1)-AR subtypes. Chirality influenced the Anticancer activity of 3 and 4 in human prostate Cancer cells (PC-3): (R)-4, eutomer at the α(1d)-AR subtype, was the most potent. The decreased effect of 4 and (R)-4 in α(1d)-AR silenced PC-3 cells confirmed that their Anticancer activity was α(1d)-AR-dependent.

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