NFB-529 is based on the ansamycin scaffold found in the natural compound geldanamycin.  The geldanamycin core structure was converted into a new, formerly unknown building block, which was consecutively used for the generation of a completely new library.  This design opens up a variety of opportunities for probing interactions with biological targets.

 

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NFI-467 is based on the indolocarbazole scaffold found in several natural compounds such as staurosporine or K252c.  The library is directed towards the ATP binding site of serine/threonine and tyrosine kinases.  Staurosporine itself is a potent kinase inhibitor, e.g. subnanomolar IC₅₀ against FLT3 kinase, with broad spectrum inhibition.  Derivatives with increased selectivity have been designed.  Staurosporine binds also to the ATP binding site of ABC multidrug transporters, indicating the potential of the indolocarbazoles to address other target classes as well.

 

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NFL-457 is based on the lupane scaffold, a pentacyclic triterpene found in natural compounds such as betulinic or platanic acid.  The scaffold is related to molecules with biological activity such as steroid hormones and cholesterol.  Dependent on the specific decoration, the lupane scaffold offers the opportunity to target diverse biological activities:  Betulinic acid shows selective cytotoxicity against melanoma cell lines and is an inducer of apoptosis.  In addition, betulinic acid inhibits HIV replication and blocks HIV entry into target cells.  While the detailed molecular mechanisms of those biological activities are unknown, it was recently shown that betulinic acid and related lupanes are agonists of nuclear hormone receptors.

 

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NFM-382 is based on the macrolactone scaffold found in the natural compound A-26771B.  Macrolactone scaffolds are found in many biologically active natural compounds, such as radicicol, borrelidin and epothilone.  The macrolactone ring serves as a core structural scaffold, which is decorated with several functional groups.  This design opens up a variety of opportunities for probing interactions with biological targets.  A-26771b itself shows a wide range of biological activity, besides antibacterial and antifungal properties the compound is known as an inhibitor of K-dependent ATPases.

 

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