Carbaboranes as pharmacophores: Similarities and differences between aspirin and asborin

• Published in: European journal of medicinal chemistry Vol. 46; no. 4; pp. 1131 - 1139
• Main Authors: Scholz, Matthias, Kaluđerović, Goran N., Kommera, Harish, Paschke, Reinhard, Will, Joanna, Sheldrick, William S., Hey-Hawkins, Evamarie
• Format: Journal Article
• Language: English
• Published: Kidlington Elsevier Masson SAS 01.04.2011; Elsevier
• Subjects: Acetates - chemistry; Acetates - pharmacology; Apoptosis - drug effects; Asborin; Aspirin; Aspirin - chemistry; Aspirin - pharmacology; Biological and medical sciences; Bones, joints and connective tissue. Antiinflammatory agents; Boron Compounds - chemistry; Boron Compounds - pharmacology; Carbaborane; Carborane; Caspases - metabolism; Catalytic Domain; Cell Line, Tumor; Cyclooxygenase 1 - chemistry; Cyclooxygenase 1 - metabolism; Cyclooxygenase 2 - chemistry; Cyclooxygenase 2 - metabolism; Cyclooxygenase 2 Inhibitors - chemistry; Cyclooxygenase 2 Inhibitors - pharmacology; Cytotoxicity; Drug Discovery; Humans; Hydrolysis; Isomerism; Medical sciences; Models, Molecular; Pharmacology. Drug treatments; Pharmacophore; Rhodamines - metabolism; Cytotoxicity; Aspirin; Carbaborane; Carborane; Asborin; Pharmacophore; Prostaglandin-endoperoxide synthase; Cage compound; Similarity; Enzyme; Enzyme inhibitor; Acetylsalicylic acid; Biological activity; Hydrolysis; Structure activity relation; Cell death; Molecular model; Boron Organic compounds; Oxidoreductases; Salicylates; Degradation product; Comparative study; Apoptosis
• ISSN: 0223-5234; 1768-3254; 1768-3254
• DOI: 10.1016/j.ejmech.2011.01.030

In medicinal chemistry carbaboranes have been used almost exclusively as boron carriers for boron neutron capture therapy (BNCT). Recent developments extended the carrier approach and use carbaboranes as scaffolds for radiodiagnostic or therapeutic agents. Most recent studies, however, focus on carb...