PASP Synthesis in the Library Production of Biologically Active Small Molecules

3 PASP Synthesis in the Library Production of Biologically Active Small Molecules 

The synthesis of an 88-membered combinatorial library 24 based upon the natural product 25 was reported by Nesterenko et al. in their search for small molecules that selectively induce apoptosis in cancer cells. The key amide bond-forming reaction was performed in parallel using a polymer-supported carbodiimide as the dehydrating agent. 

Other examples of arrays of biologically active compounds accessed through a multi-step RASP approach, include the synthesis of cysteine protease inhibitors by Ellman, and Armstrong s synthesis of a 25-membered array of analogues of the breast cancer drug Tamoxifen.  

The use of PASP synthesis in medicinal chemistry programmes to date has been extensively exploited by Parlow et previously at Pharmacia, in their search 

3 Automated PASP Synthesis of Biologically Active Molecules 

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