Chromopynones are pseudo natural product glucose uptake inhibitors targeting glucose transporters GLUT-1 and -3

Karageorgis G, Reckzeh ES, Ceballos J, Schwalfenberg M, Sievers S, Ostermann C, Pahl A, Ziegler S, Waldmann H (2018). Nat Chem. 

doi: 10.1038/s41557-018-0132-6. 

The Waldmann lab developed a novel concept to  overcome the limits of the design and synthesis of bioactive compounds.They therefore combined natural product (NP)-derived fragments to structurally unprecedented „pseudo natural products“.

They provide a proof o principle by designing, synthesizing and investigating the biological properties of chromopynone pseudo NPs that combine biosynthetically unrelated chromane and tetrahydropyrimidinone NP fragments. The developed chromopynones define a glucose uptake inhibitor chemotype that selectively targets glucose transporters GLUT-1 and -3. 

More information on the design of pseudo natural products here: Nature 2.0 – Inspiring new drug discovery by pseudo natural products

Design of chromopynone pseudo NPs.
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