Platinum-based drugs, mainly cisplatin, are employed for the treatment of solid malignancies. However, cisplatin treatment often results in the development of chemoresistance, leading to therapeutic failure. Here, the antitumor activity of different trans-sulfonamide platinum complexes in a panel of human cell lines is presented. The cytotoxicity profiles and cell cycle analyses of these platinum sulfonamide complexes were different from those of cisplatin. These studies showed that complex 2b with cyclohexyldiamine and dansyl moieties had the best antitumoral activities.
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| http://dx.doi.org/10.1016/j.ejmech.2014.02.022 | DOI Listing |
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Evaluation of novel trans-sulfonamide platinum complexes against tumor cell lines.
Eur J Med Chem
April 2014
Medical Oncology Service, Hospital Universitario 12 de Octubre, Avda de Córdoba S/N, 28041 Madrid, Spain; Instituto de Investigación Hospital 12 de Octubre, Avda de Córdoba S/N, 28041 Madrid, Spain. Electronic address:
Platinum-based drugs, mainly cisplatin, are employed for the treatment of solid malignancies. However, cisplatin treatment often results in the development of chemoresistance, leading to therapeutic failure. Here, the antitumor activity of different trans-sulfonamide platinum complexes in a panel of human cell lines is presented.
View Article and Find Full Text PDFExpanding the synthesis of new trans-sulfonamide platinum complexes: cytotoxicity, SAR, fluorescent cell assays and stability studies.
J Inorg Biochem
October 2013
Departamento de Química Inorgánica (Módulo 7), Facultad de Ciencias, Universidad Autónoma de Madrid, 28049, Madrid, Spain.
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.
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