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.

combretastatin

 

Bioorganic and Medicinal Chemistry Link

Advertisements

Leave a Reply

Fill in your details below or click an icon to log in:

WordPress.com Logo

You are commenting using your WordPress.com account. Log Out /  Change )

Google photo

You are commenting using your Google account. Log Out /  Change )

Twitter picture

You are commenting using your Twitter account. Log Out /  Change )

Facebook photo

You are commenting using your Facebook account. Log Out /  Change )

Connecting to %s

 
%d bloggers like this: