Design, synthesis, and biological evaluation of prazosin-related derivatives as multipotent compounds

  • J Med Chem. 2005 Jan 13;48(1):28-31. doi: 10.1021/jm049153d.
Alessandra Antonello  1 ,  Patrizia Hrelia ,  Amedeo Leonardi ,  Gabriella Marucci ,  Michela Rosini ,  Andrea Tarozzi ,  Vincenzo Tumiatti ,  Carlo Melchiorre
Affiliations
  • 1. Departments of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
PMID: 15633998 DOI: 10.1021/jm049153d
Abstract

To combine in the same molecule alpha(1)-adrenoreceptor blocking and antioxidant properties, compounds 2-5 were designed and synthesized. All compounds were effective alpha(1)-adrenoreceptor antagonists and were tested in both functional and binding assays. In addition, compounds 2 and 5 also displayed significant capacity to inhibit intracellular oxidative stress, whereas 3-5 exerted potent antiproliferative activity in lymph node carcinoma of prostate cells.