Research Highlights

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Published online: 3 February 2010 | doi:10.1038/nchina.2010.15

Medicinal chemistry: Changing targets

Anne Pichon

Introduction

© (2010) RSC

The platinum-based compound cisplatin is a powerful drug against testicular and ovarian cancers, but it has limited use against other types of cancer. Zijian Guo and co-workers at Nanjing University¹ have now created a series of complexes that specifically target human osteosarcoma by incorporating bone-seeking moieties onto a cisplatin derivative.

Phosphonate (PO₃) is a compound with bone-targeting properties. Previous studies have successfully attached PO₃ moieties to the platinum centre of cisplatin. However, these moieties often detach during the complicated physiological process — well before cisplatin could reach the bone tumour.

The researchers prepared four complexes by attaching bisphosphonate moieties to a side group (instead of the platinum centre) of the cisplatin-based drug. Bisphosphonate comprises two PO₃ groups and a side chain covalently linked to a common carbon atom. The side chain securely fastens the bisphosphonate moieties to the cisplatin.

The complexes exhibit excellent solubility in both organic and aqueous solutions, and cytotoxicity assays showed that two of these complexes are lethal against the human osteosarcoma cell line. The findings demonstrate an approach for using cisplatin against a wide range of cancers.

The authors of this work are from:
State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing, China; State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, China.

Reference

1. Xue, Z. et al. Platinum(II) compounds bearing bone-targeting group: synthesis, crystal structure and antitumor activity. Chem. Commun. doi:10.1039/b922222g (2010). | Article