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Synthesized for the first time! Redefining the treatment landscape for the 'silent killer,' marine anti-cancer molecules usher in the dawn of a 'simplified version' of new drugs

2025-12-24


Ovarian cancer is known as the 'silent killer' due to the hidden nature of its early symptoms, and most patients are already in the late stages when diagnosed, resulting in a long-term low survival rate. Against this backdrop, marine natural products have become a new direction for anticancer drug development. In 2010, scientists isolated a structurally complex molecule, Gukulenin A, from a sponge species in Korean waters, and experiments showed its potential against ovarian cancer. However, the molecule contains two unstable tropolone rings and multiple chiral centers, making its synthesis extremely challenging, and it had not been artificially replicated for fourteen years.  

Recently, a research team from Yale University and other institutions published a paper in Science, reporting the first successful total synthesis of Gukulenin A. The team designed a modular synthesis route requiring only 24 steps and created 15 analogs. Through activity testing, they identified the key structures responsible for its anticancer effects—the dual tropolone rings and the aldehyde group are indispensable, while other parts can be simplified or modified. This discovery provides an important foundation for the subsequent development of simpler and more stable candidate drugs against ovarian cancer.


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