Cancer cell cytotoxicity of cyclometalated compounds obtained with osmium(II) complexes.

Abstract

A library of 29 organoosmium compounds has been built up with known and novel cyclometalated compounds obtained with C-N, N(∧)C(∧)N, and C(∧)N(∧)N ligands. All compounds have been tested for their in vitro cytotoxic properties against A172, a tumor cell line derived from a human glioblastoma, this affording a contrasted picture of the activities of the compounds gathered in this study. Some compounds displayed good to excellent activities, some of them showing IC50 in the nanomolar range. The level of activity was tentatively correlated to several physicochemical properties of the compounds such as their E(0)1/2(Os(III/II)) redox potential and their lipophilicity (log Po/w). A parallel with related ruthenium derivatives was tentatively proposed.

• Authors: Bastien Boff, Christian Gaiddon, Michel Pfeffer
• Journal: Inorganic chemistry (Inorg Chem) Vol. 52 Issue 5 Pg. 2705-15 (Mar 04 2013) ISSN: 1520-510X [Electronic] United States
• PMID: 23427955 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Organometallic Compounds
• Osmium

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor
• Humans
• Models, Molecular
• Molecular Structure
• Organometallic Compounds (chemical synthesis, chemistry, pharmacology)
• Osmium (chemistry)
• Structure-Activity Relationship