Parallel synthesis and biological screeening of pyrazole and pyrimidine analogs

ORGN 567

John Nielsen, jn@kvl.dk, Tobias Persson, tp@kvl.dk, and Jakob E. Rasmussen. Department of Natural Sciences, Bioorganic Chemistry Section, The Royal Veterinary and Agricultural University, Thorvaldsensvej 40, DK-1871 Frederiksberg C, Denmark
Pyrazoles and pyrimidines are heteroaromatic structures with a common synthetic origin in two synthons, 1,3-dielectrophiles and dinucleophiles. A recent discovery in our research group was the synthesis of β-enaminoketoesters in one step and that these 1,3-dielectrophiles can be used in cyclocondensations. We have explored β-enaminoketoesters as intermediates in the synthesis of ester-functionalized heterocycles and analogs thereof through further functionalizations. The pyrazole and pyrimidine scaffolds display diverse biological activities and the specific target of our biological screening was protein kinases for which the observed bioactivities will be presented.