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Harvard Chemist's Developed Synthesis Advance Potent Anti-Malignant Tumour Agent

Harvard University chemist's synthesis of halichondrin is known to be a potent anti-cancer agent.

Harvard University Chemists have achieved a landmark in drug discovery spending three decades in making it. Synthesis of halichondrin of molecules known as anti-cancer agent in mouse studies, found naturally in sea sponges in minuscule quantities.

A research team led by Yoshito Kishi, Morris Loeb Professor of chemistry emeritus in Harvard University Synthesised sufficient quantities of E7130.

A drug candidate from the hailchondrin class, enabled its biological activity, pharmacological properties and efficacy for the first time along with the researchers at Japanese pharmaceutical company Eisai.

Under the license of Harvard's Office of Technology Development (OTD), clinical trial Eisai, Japan tested the molecule under the Phase I, the molecule had undergone a rapid development.

The company hopes to begin a second clinical trial in the US in the due course. After a three-year research at Kishi Lab in collaboration with Eisai they released a scientific report.

The paper reports the total synthesis of the highly potent hailchondrin molecule E7130, 11.5 grams of it, with 99.81 per cent purity and characterises its mode of action. In the preclinical studies, they identified it as not only a microtubule dynamics inhibitor, but also as a novel agent to target the tumour microenvironment.

The structure of the complete E7130 molecule derived by total synthesis is particularly challenging to replicate because it has 31 chiral centre's, asymmetrical points that must each be correctly oriented. In other words, there are roughly 4 billion ways to get it wrong.

The team's results of studies conducted in vitro and in vivo, in animal models that shed light on the molecule's complex mode of action. The team showed that E7130 can increase intratumoural CD31-positive endothelial cells and reduce alpha-SMA-positive associates of fibroblasts, components of the tumor microenvironment that may be involved in the transformation to malignancy.

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