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Analogues of zampanolide: Design, synthesis and anti-cancer activity

42 months
Approved budget:
Dr Joanne Harvey
Health issue:
Cancer (oncology)
Proposal type:
Emerging Researcher First Grant
Lay summary
Anti-cancer drugs generally act to disrupt chemical processes inside cancer cells that allow them to divide into new cells. Microtubules, which form the framework of the cell division machinery, have proven to be clinically important drug targets. Zampanolide is a microtubule-targeting agent that was discovered in marine sponges. It is important to make and evaluate structural variants of zampanolide because natural compounds are not, in general, optimised for human cancer therapy. Such analogues will increase our knowledge of the way the natural compound works and allow us to improve on the anti-cancer function through the design and synthesis of further analogues. We will design analogues of zampanolide using information we have obtained about its interactions with the tubulin binding sites. These analogues will be synthesised in the lab and then tested against human cancer and immune cells in order to determine their potential as cancer therapeutics.