Research in our group has focused on the synthesis of several different types of protein kinase inhibitors.  A recent emphasis has been synthesis of 3,6-disubstituted pyrazolo[1,5-a]-pyrimidines a molecular scaffold known to inhibit VEGFR2, a receptor tyrosine kinase (RTK) overexpressed in a variety of cancers.  We have prepared several 3,6-disubstituted pyrazolo[1,5-a]-pyrimidines using a microwave assisted approach that greatly streamlines the previously published synthesis.    We will present background information relative to the known antiangiogenic activity of this class of compounds together with an overview of the progress we have made in preparing new analogues.   Two of our analogues selectively inhibited melanoma cell line MDS-MB-435 and leukemia cell lines K-562 and SR by 50-70% at 10 uM concentration. <br/>

Microwave-assisted synthesis of 3,6-disubstituted pyrazolo[1,5-a]-pyrimidines and progress toward discovery of anticancer activities

2019 Fall National Meeting

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