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Synthesis and anticancer activity of a new water-soluble derivative of heptaplatin, cis-{Pt(II)[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane](3-acetoxyl-cyclobutane-1,1-dicarboxylato)}

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Abstract

A new water-soluble derivative of heptaplatin, cis-{Pt(II)[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane](3-acetoxyl-cyclobutane-1,1-dicarboxylato)} has been synthesized, characterized by elemental analysis, MS, IR, and 1H, 13C NMR, and evaluated for in vitro anticancer activity in four human cancer cell lines. The stability of the derivative in water was also investigated by monitoring the changes of 1H NMR in D2O. The results reveal that the new derivative has good solubility and stability in water and also shows high anticancer activity against gastric cancer cells, ovarian cancer cells, and colon cancer cells. Therefore, it is worthy of further evaluation for in vivo antitumor activity and toxicity.

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Acknowledgments

The authors are grateful to the National Science Foundation of P. R. China (Grant No. 21161010) and China National Research and Development Program (Grant No. 2012BAE06B08) for financial support.

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Correspondence to Wei-Ping Liu.

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Jiang, J., Lei, J., Chen, XZ. et al. Synthesis and anticancer activity of a new water-soluble derivative of heptaplatin, cis-{Pt(II)[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane](3-acetoxyl-cyclobutane-1,1-dicarboxylato)}. Res Chem Intermed 41, 6149–6155 (2015). https://doi.org/10.1007/s11164-014-1728-0

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