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Chemistry breakthroughs open new doors to drug developers and cancer researchers

Posted February 5, 2018

Two independent chemistry breakthroughs have opened a plethora of doors that were previously locked to drug developers and cancer researchers.

The discoveries, which involved adding new materials to a previously unstable chemical scaffold and building molecules onto the “pigments of life”, will also offer new possibilities to molecular engineers, materials and computer scientists, and energy researchers.

Credit: Pixabay

Thinking inside the box

In the first case, scientists solved a decades-old challenge by developing new tools for a synthetic (man-made) molecule – cubane – that is widely used in the pharma industry. Cubane molecules consist of eight carbon atoms arranged at the corners of a perfect cube. Yet despite the simplicity of the shape, modern chemistry has, until now, had a very tough time handling its unique reactivity. By deciphering how to circumvent this inherent reactivity, the door is now open for drug developers to create new, more diverse therapeutics from cubane and its derivatives.

The scientists were led by a team from Trinity College Dublin’s School of Chemistry. Their discovery was recently published in the international journal Chemistry – A European Journal, in which it features as a VIP paper and on the journal front cover.

A team of six researchers under the supervision of Professor of Organic Chemistry at Trinity, Mathias O. Senge, discovered how to circumvent the inherent reactivity of the cubane core, while Senior Research Fellow, Dr Bernhard, and the other team members essentially filled the empty cubane toolbox, which allowed them to establish new connections and craft important residues onto the cubane scaffold.

Professor Senge said: “I often challenge my students to think outside the box so I was really surprised when they pitched the idea of thinking inside the box. However, it is the apparent simplicity of the cubane core that really underlies the impact of the present accomplishment.”

“We have a structurally unique building block which has been neglected by the majority of synthetic chemists up to now, precisely because this cube is so difficult to work with. However, with great risk comes great reward. I am delighted with our present success and intrigued about the avenues it will open in fields ranging from new drug discovery to 21st century computer chip generation!”

“The results from this long-term, fundamental research project will have significant benefits in the years to come as we can now prepare a greater variety of tailored compounds. We are very grateful to have received continuous long-term funding from Science Foundation Ireland to support this work, without which we would not have made this important discovery.”

Source: Trinity College Dublin

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