title: Design, synthesis, and biological evaluation of prazosin-related derivatives as multipotent compounds.
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.
authors.affiliation: Departments of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Antonello
authors.forename: Patrizia
authors.initials: P
authors.lastname: Hrelia
authors.forename: Amedeo
authors.initials: A
authors.lastname: Leonardi
authors.forename: Gabriella
authors.initials: G
authors.lastname: Marucci
authors.forename: Michela
authors.initials: M
authors.lastname: Rosini
authors.forename: Andrea
authors.initials: A
authors.lastname: Tarozzi
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Tumiatti
authors.forename: Carlo
authors.initials: C
authors.lastname: Melchiorre
mesh_terms: D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001671:Biochemistry / Q000379:methods; D016466:CHO Cells; D002277:Carcinoma / Q000188:drug therapy; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D011224:Prazosin / Q000031:analogs & derivatives* / Q000737:chemistry; D011471:Prostatic Neoplasms / Q000188:drug therapy; D051381:Rats; D017382:Reactive Oxygen Species; D018340:Receptors, Adrenergic, alpha-1 / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D008063:Thioctic Acid / Q000737:chemistry / Q000494:pharmacology; D014407:Tumor Cells, Cultured; D014649:Vas Deferens / Q000187:drug effects
chemical_list: D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D000975:Antioxidants; D017382:Reactive Oxygen Species; D018340:Receptors, Adrenergic, alpha-1; D008063:Thioctic Acid; D011224:Prazosin