Dublin: Titanocene derivatives show anti-tumour effect in preclinical models

05 Feb 2008 | News

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Matthias Tacke and his research team at the Centre for Synthesis and Chemical Biology and the School of Chemistry and Chemical Biology at University College Dublin published highly significant preclinical results on the anti-tumour activity of titanocene Y on human breast tumours and in a mouse model.

In the mouse model, a decrease not only in tumour growth but also a reduction in tumour volume to around one-third was observed for the first time. In the human breast cancer cells titanocene Y showed cell death induction comparable to the widely used chemotherapy drug Cisplatin.

Tacke’s group has been working on anti-cancer drugs belonging to the titanocene family for five years. 25 novel compounds were initially synthesised in the lab, and were structurally identified and then biologically evaluated.

The most successful analogues so far, titanocene X and titanocene Y, have been shown in early in-vitro and ex-vitro experiments to target prostrate, cervix and renal cell cancers, as well as breast cancer cell lines. The researchers believe that titanocenes represent a novel series of promising antitumour agents.

Tacke said, “The successor molecule has been synthesised and has been shown to be 13 times more cytotoxic in vitro. Investigations of this candidate in the next mouse model are currently under way.”

The UCD compounds are derivatives of titanocene dichloride, which has previously failed in phase II clinical trials carried out in Germany in 1998. The UCD team has focused on developing effective derivatives.


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