Abstract
A platinum (II) complex stabilized by a pyridine and an N-heterocyclic carbene ligand featuring an anthracenyl moiety was prepared. The compound was fully characterized and its molecular structure was determined by single-crystal X-ray diffraction. The compound demonstrated high in vitro antiproliferative activities against cancer cell lines with IC50 ranging from 10 to 80 nM. The presence of the anthracenyl moiety on the N-heterocyclic carbene (NHC) Pt complex was used as a luminescent tag to probe the metal interaction with the nucleobases of the DNA through a pyridine-nucleobase ligand exchange. Such interaction of the platinum complex with DNA was corroborated by optical tweezers techniques and liquid phase atomic force microscopy (AFM). The results revealed a two-state interaction between the platinum complex and the DNA strands. This two-state behavior was quantified from the different experiments due to contour length variations. At 24 h incubation, the stretching curves revealed multiple structural breakages, and AFM imaging revealed a highly compact and dense structure of platinum complexes bridging the DNA strands.
Highlights
Inorganic compounds have an enormous impact in medicine, in the treatment of cancer
A summary of crystal and refinement data is included in complex displays the coordination of the pyridine ligand trans to the N-heterocyclic carbene ligand structure of the N-heterocyclic carbenes (NHC)
We have shown that a platinum diiodo complex stabilized by a pyridine and an N-heterocyclic carbene ligand featuring an anthracenyl moiety has high in vitro antiproliferative activities against several cancer cell lines, with IC50 values below 100 nM
Summary
Inorganic compounds have an enormous impact in medicine, in the treatment of cancer. Since Rosenberg’s [1,2] discovery of the cytotoxicity of cisplatin, it has found wide use as a chemotherapeutic in clinics and cisplatin continues to be used in 50–70% of all patients suffering cancer, usually administered with other drugs in combination therapy [3]. It is especially effective in treating testicular [4] and ovarian [5] carcinoma but is used to treat other types of cancers [6].
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