Researchers at the Massachusetts Institute of Technology (MIT) have announced the first successful synthesis of a complex fungal compound called Verticillin A, more than 50 years after it was discovered. The compound has long been viewed as a potential anti-cancer agent.

Verticillin A has an intricate structure, which has made it difficult to synthesize. Researchers explained that subtle changes in its molecular structure significantly increased the challenge.

“We now have the technology to access Verticillin A for the first time and create many designed variants,” said Mohammad Movassaghi, a Professor of Chemistry at MIT. “This will enable further detailed studies.”

In laboratory tests on human cancer cells, a derivative of Verticillin A showed promise against diffuse midline glioma, a type of pediatric brain cancer.

Jun Qi, Associate Professor of Medicine at Dana-Farber Cancer Institute/Boston Children’s Cancer and Blood Disorders Center and Harvard Medical School, revealed that the research is part of ongoing efforts to explore natural compounds for drug development.

The synthesis required precisely fusing two identical halves into a dimer with the correct three-dimensional arrangement. Researchers used a 16-step process that included reordering bond-forming events and protecting fragile molecular bonds.

Movassaghi reported that timing was critical in the process. “We had to significantly change the order of the bond-forming events to succeed,” he said.

The study was published in the Journal of the American Chemical Society. Scientists now plan to study how Verticillin A interacts with cancer cells and explore its therapeutic potential.

Key points:

• MIT researchers successfully synthesized Verticillin A for the first time.
• The compound shows potential against pediatric diffuse midline glioma.
• The process involved a precise 16-step chemical synthesis.

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