ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

Synthesis, molecular characterisation, and in vivo study of platinum(IV) coordination compounds against B16 mouse melanoma tumours

Iwona Łakomska, Anna Kaźnica, Romana Joachimiak, Andrzej Marszałek and Jerzy Sitkowski, Lech Kozerski, and Tomasz Drewa

Faculty of Chemistry, Nicolaus Copernicus University, Gagarina 7, 87-100 Toruń, Poland

E-mail: dziubek@umk.pl

Abstract: A novel platinum(IV) coordination compound with 6-mercaptopurine (6-Hmp) has been synthesised and characterised by IR and NMR spectroscopy. Spectroscopic parameters indicate the presence of two chelate (S-6, N-7) monodeprotonated ligands and two chloride ions in the coordination sphere of [PtCl₂(6-mp)₂] · H₂O (I). Two Pt(IV) coordination compounds, [PtCl₂(6-mp)₂] · H₂O (I) and [PtCl₄(dbtp)₂] (II), were used in the in vivo test against B16 mouse melanoma tumours. Cytotoxic activity of compound II against the tumour cells was found to be high (LC₁₀ = 2.6 μM, LC₅₀ = 17.0 μM, LC₉₀ = 58.0 μM) compared to that of cisplatin.

Keywords: platinum(IV) complexes – purine analogues – NMR – cytotoxicity in vivo – melanoma

Full paper is available at www.springerlink.com.

DOI: 10.2478/s11696-011-0019-0

Chemical Papers 65 (3) 308–314 (2011)