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Merck

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

Journal of medicinal chemistry (2005-01-07)
Alessandra Antonello, Patrizia Hrelia, Amedeo Leonardi, Gabriella Marucci, Michela Rosini, Andrea Tarozzi, Vincenzo Tumiatti, Carlo Melchiorre
RESUMO

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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(R)-(+)-α-Lipoic acid, analytical standard