Natural product libraries activity range

Natural product library Varies Biological activity, wide range of different pharmacophores Difficult to synthesize, difficult to obtain pure compound, target identification is challenging Prestwick, Enzo Lifesciences, Microsource... 

In addition to natural product sources, chemical compound libraries are used frequently in the drug discovery process. These libraries can range from small, focused libraries specifically synthesized with a particular target in mind to massive, randomly generated libraries. While there is still the problem of deconvolution of an active library, synthetically generated libraries do have a few advantages over natural product extract mixtures. There are typically equal... 

A number of examples such as 1,3-dioxanes, macrolactones, °° ring-containing biaryls, ° spirooxindoles, alkaloid-like compounds, and polycyclic compounds from the Schreiber group illustrate this approach to natural product-like libraries (see Chapter 11). An early example converted shikimic acid into intermediate tetracyclic y-butyrolactones, which were then functionalized around the core structure (see Chapter 11, Subsection 11.10.2). y-Butyrolactones, found in about 10% of all natural products and which exhibit a broad range of biological activities, are a key element in a number of recent natural product-like compounds. A more recent example, inspired by the rich skeletal diversity of indole alkaloids, utilized the rhodium(II)-catalyzed consecutive cyclization-cycloaddition reactions developed by Padwa and coworkers (Scheme 1.4). A stereocontrolled tandem reaction utilizing the versatile scaffold allowed for multiple modes of intramolecular reactions. 

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