2. Academic Validation
  3. Design, synthesis, and biological evaluation of prazosin-related derivatives as multipotent compounds

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

Affiliation

  • 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.

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