Naturalproductman’s Blog

Hey, is that a natural product?!

Combretastatin Analogs

Posted by naturalproductman on November 2, 2009

Sylvie Duckie and co-workers at UMIST in Manchester have recently published in Bioorganic and Medicinal Chemistry on biological and synthetic studies of chalcone analogs.  The most amazing properties had to do with the IC50s of the K562 human chronic myelogenous leukemia cell line.  Some of the substrates that were made possessed sub-nanomolar IC50s.  If you look at the substrates carefully, then you should know well enough that these are dienones that are excellent Nazarov cyclization precursors.  These substrates were based off of a natural product, combretastatin A4, that had anti-tubulin polymerization activity by binding to the colchicine binding site belonging to the beta-tubulin subunit.



Bioorganic and Medicinal Chemistry Link

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