Synthesis, crystal structure and cytotoxicity studies of cis-dichloro(4,5-diazafluoren-9-one)platinum(II)

• The molecular structure of cis-Pt(dafone)Cl2 has been determined.
• Dafone, unlike in most of its known complexes, forms symmetrical chelate bonds in the Pt(II) complex.
• This complex binds covalently to DNA and has a cytotoxic activity comparable to that of cis-platin.

cis-Pt(dafone)Cl2 has been synthesized and crystallographically characterized. Dafone, in spite of its long chelate bite, binds in a symmetrical fashion with longer Pt–N distances compared to its phen (1,10-phenanthroline) and bipy (2,2′-bipyridine) analogs. The covalent binding of the complex with DNA was explored by absorption and emission spectroscopy, and electrophoretic mobility shift assay. Cytotoxicity studies of the complex against human cervical carcinoma cells (HeLa) and immortal human keratinocyte (HaCat) cell lines indicate that it has an activity comparable to that of the famed drug, cis-platin.

Dafone forms symmetrical chelate bonds in cis-Pt(dafone)Cl2. The covalent binding to DNA and cyotoxicity of this cis-platin analog is evaluated.Figure optionsDownload as PowerPoint slide