Four water-soluble dia(m)mine platinum complexes with 3-oxo-cyclobutane- 1,1-dicarboxylate as the leaving group have been synthesized. These compounds were evaluated for their in vitro anticancer activity against three human A549, SK-OV-3, and HT-29 cancer cell lines. All the tested compounds showed potent activity in lung carcinoma (A549), ovarian carcinoma (SK-OV-3), and colon cancer cell (HT-29) lines. Complex 2(IC50 value = 1.57 µM for A549 and IC50 value = 0.88 µM for HT-29 cells) and Complex 4 (IC50 value = 15.3 µM for SK-OV-3 cells) displayed the most potent anticancer activity of the series. Also, preliminary acute toxicity of the platinum complexes derivatives has shown the same level as carboplatin and lower toxicity than cisplatin in vivo. All the complexes were characterized by elemental analysis as well as by ESI+-MS, FT-IR, 1H- and 13C-NMR, and have shown a satisfactory water solubility.
Research on Chemical Intermediates – Springer Journals
Published: Feb 1, 2015
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