Expanding the synthesis of new trans-sulfonamide platinum complexes: Cytotoxicity, SAR, fluorescent cell assays and stability studies

• Published in: Journal of inorganic biochemistry Vol. 127; pp. 128 - 140
• Main Authors: del Solar, Virginia, Quiñones-Lombraña, Adolfo, Cabrera, Silvia, Padrón, José M., Ríos-Luci, Carla, Alvarez-Valdés, Amparo, Navarro-Ranninger, Carmen, Alemán, José
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.10.2013
• Subjects: Biological Assay; Cell Line, Tumor; Cell Proliferation - drug effects; Coordination Complexes - chemical synthesis; Coordination Complexes - chemistry; Coordination Complexes - pharmacology; Drug Screening Assays, Antitumor; Drug Stability; Fluorescence; Fluorescent assays; Humans; Platinum - chemistry; Quinoxalines - chemistry; Quinoxalines - pharmacology; SAR; Structure-Activity Relationship; Sulfanilamides - chemistry; Sulfanilamides - pharmacology; Sulfonamides; Sulfonamides - chemistry; Sulfonamides - pharmacology; Trans-platinum complexes; Trans-platinum complexes; Fluorescent assays; Sulfonamides; SAR
• ISSN: 0162-0134; 1873-3344
• DOI: 10.1016/j.jinorgbio.2013.01.013

In this manuscript, we describe the synthesis of new trans-N-sulfonamide platinum complexes and their antiproliferative activity (GI50, μM) in human solid tumors cells. The structure activity relationships (SAR), with different new synthesized complexes by variation in ligand, halogen and also in the stereochemistry of the ligand, has been studied. Solubility and stability studies have also been carried out as well as fluorescent cell assays in order to clarify the final target in the tumor cells. [Display omitted] ► Synthesis of new trans-platinum complexes containing sulfonamides. ► A structure activity relationship is studied. ► Fluorescent cell assays were studied to clarify the final target in the tumor cells.