Synthesis of Pt(II) complexes of the type [Pt(1,10-phenanthroline)(SArF)] (SArF = SCH-3,4-F; SCF-4-H; SCF). Preliminary evaluation of their in vitro anticancer activity.

A series of Pt(II) complexes of the type [Pt(1,10-phenanthroline)(SArF)] (SArF = SCH-3,4-F(1); SCF-4-H (2); SCF(3)) were synthesized from [Pt(1,10-phenanthroline)(Cl)] and [Pb(SArF)] via metathesis reactions. The complexes were fully characterized including the unambiguous determination of their molecular structures by single-crystal X-ray diffraction techniques, showing the metal centers to be into a slightly distorted square-planar environments. The in vitro cytotoxic activity of the complexes was evaluated on six cancerous cell lines, i.e: glial cells of nervous central system (U-251), prostate (PC-3), leukemia (K-562), colon (HCT-15), breast (MCF-7) and lung (SKLU-1); we also included a healthy cell line of COS-7 (African green monkey kidney) for comparative purposes. We found that complex 2 was selective for PC-3. In addition, the IC values for the series of complexes were determined using the U-251, HCT-15 and SKLU-1 cancerous cell lines, as well as in the healthy cell line (COS-7), where complex 1 exhibited the best activity, with IC values going from 4.56 to 4.78 μM. These studies where further complemented with DNA docking theoretical calculations and DNA affinity experiments.