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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Adrenergic alpha-1 Receptor Antagonists
-
Adrenergic alpha-Antagonists / chemical synthesis
-
Adrenergic alpha-Antagonists / chemistry*
-
Adrenergic alpha-Antagonists / pharmacology*
-
Animals
-
Antioxidants / chemical synthesis
-
Antioxidants / chemistry*
-
Antioxidants / pharmacology*
-
Biochemistry / methods
-
CHO Cells
-
Carcinoma / drug therapy
-
Cricetinae
-
Cricetulus
-
Drug Design
-
Drug Evaluation, Preclinical / methods
-
Humans
-
In Vitro Techniques
-
Male
-
Prazosin / analogs & derivatives*
-
Prazosin / chemistry
-
Prostatic Neoplasms / drug therapy
-
Rats
-
Reactive Oxygen Species
-
Receptors, Adrenergic, alpha-1 / genetics
-
Receptors, Adrenergic, alpha-1 / metabolism
-
Structure-Activity Relationship
-
Thioctic Acid / chemistry
-
Thioctic Acid / pharmacology
-
Tumor Cells, Cultured
-
Vas Deferens / drug effects
Substances
-
Adrenergic alpha-1 Receptor Antagonists
-
Adrenergic alpha-Antagonists
-
Antioxidants
-
Reactive Oxygen Species
-
Receptors, Adrenergic, alpha-1
-
Thioctic Acid
-
Prazosin