NDLI: Structure, solution chemistry, antiproliferative actions and protein binding properties of non-conventional platinum(II) compounds with sulfur and phosphorus donors

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Messori, Luigi Beyer, Antje Casini, Angela Weigand, Wolfgang Rothenburger, Claudia Landini, Ida Görls, Helmar Gabbiani, Chiara Mügge, Carolin Nobili, Stefania Mini, Enrico Michelucci, Elena
Description	Author Affiliation: Mügge C ( Institute of Inorganic and Analytical Chemistry, Friedrich-Schiller-University Jena, August-Bebel-Strasse 2, 07743, Jena, Germany.)
Abstract	Twelve Pt(II) complexes with $cis-PtP_{2}S_{2}$ pharmacophores (where $P_{2}$ refers to two monodentate or one bidentate phosphane ligand and $S_{2}$ is a dithiolato ligand ) were prepared, characterized and evaluated as potential antiproliferative agents. The various compounds were first studied from the structural point of view; afterward, their solubility properties as well as their solution behaviour were analyzed in detail. Antiproliferative properties were specifically evaluated against A2780 human ovarian carcinoma cells, either resistant or sensitive to cisplatin. For comparison purposes similar studies were carried out on four parent cis-dichloro bisphosphane Pt(II)complexes. On the whole, the $cis-PtP_{2}S_{2}$ compounds displayed significant antiproliferative properties while the $cis-PtP_{2}Cl_{2}$ (cis-dichloro bisphosphane Pt(II)) compounds revealed quite poor biological performances. To gain further insight into the molecular mechanisms of these bisphosphane Pt(II) compounds, the reactions of selected complexes against the model protein cytochrome c were investigated by ESI-MS and their adduct formation explored. A relevant reactivity with cyt c was obtained only for $cis-PtP_{2}Cl_{2}$ compounds, whereas $cis-PtP_{2}S_{2}$ compounds turned out to be nearly unreactive. The obtained results are interpreted and discussed in the frame of the current knowledge of anticancer platinum compounds and their structure–activity-relationships. The observation of appreciable antiproliferative effects for the relatively inert $cis-PtP_{2}S_{2}$ compounds strongly suggests that these compounds will undergo specific activation within the cellular environment.
ISSN	14779226
Issue Number	9
Volume Number	40
e-ISSN	13645447
Journal	Dalton Trans.
Language	English
Publisher	Royal Society of Chemistry
Publisher Date	2011-03-07
Publisher Place	Great Britain (UK)
Access Restriction	Subscribed
Subject Keyword	Antineoplastic Agents Chemistry Chemical Synthesis Cell Proliferation Drug Effects Platinum Compounds Sulfur Cell Line, Tumor Cisplatin Toxicity Cytochromes c Female Humans Ligands Magnetic Resonance Spectroscopy Methods Molecular Structure Organoplatinum Compounds Ovarian Neoplasms Drug Therapy Phosphines Phosphorus Protein Binding Spectrophotometry, Ultraviolet Structure-Activity Relationship Journal Article Research Support, Non-U.S. Gov't
Content Type	Text
Resource Type	Article
Subject	Inorganic Chemistry

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