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Synthesis and cytotoxic activity of new Pt (II) complexes with nitropyrazoles in aerobic and hypoxic conditions

Andrzej Regiec 1Henryk Mastalarz 1Joanna Wietrzyk 2Stanisław Ryng 1

1. Wrocław Medical University, Faculty of Pharmacy, Department of Organic Chemistry, Grodzka 9, Wrocław 50-137, Poland
2. Polish Academy of Sciences, Institute of Immunology and Experimental Therapy (IITD), Rudolfa Weigla 12, Wrocław 53-114, Poland


Hypoxic conditions are usually the common feature of solid tumors resulting from their inefficient microvascular systems due to the rapid tumor growth  [1]. This behavior distinguished solid tumor cells from normal cells causing their resistance to the chemo- and radiotherapy but, on the other hand, also giving new opportunities for selective cancer treatment. In our approaches to the design and synthesis of targeted anticancer prodrugs for tumor site-specific activation we paid our attention to Pt(II) complexes with nitrodiazoles. This class of compounds potentially should exhibit dual mode of action, binding to DNA and undergo the bioreductive activation process.

On presented poster, the synthesis of new platinum complexes with nitropyrazoles and their cytotoxic activity against tumor line cells in aerobic and hypoxic conditions [2] is going to be shown. Revealed activity of tested complexes shows strong cytotoxic activity of new platinum complexes against tumor lines, in a few cases, stronger than reference drug cisplatin.

Research was granted by KBN financial support,  grant nr N N401 052938


1.  Chen Y., Hu L., Design of anticancer prodrugs for reductive activation, Med. Res. Rev., 2009 Jan;29(1), 29-64

2.  Andrzej Regiec, Agnieszka Mastalarz, Henryk Mastalarz, Joanna Wietrzyk, Cis- i trans- związki kompleksowe platyny(II) z 1-metylo-4-nitropirazolem, sposób ich wytwarzania, rozdzielania, izomeryzacji i zastosowanie do wytwarzania leków do terapii przeciwnowotworowej, zgłoszenie patentowe (patent application) nr P.393483, 2010



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Related papers

Presentation: Poster at VIII Multidyscyplinarna Konferencja Nauki o Leku, by Andrzej Regiec
See On-line Journal of VIII Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2012-03-14 11:29
Revised:   2012-03-15 10:42