Physical Sciences and Mathematics Commons^™

Synthesis Of An Archazolid Based Enzyme Inhibitor, Cooper A. Vincent

WWU Graduate School Collection

The archazolids are a family of natural products that display powerful growth inhibitory activity against a number of human cancer cell lines. This activity has been linked to inhibition of the vacuolar-type ATPase (V-ATPase) and more recently cyclooxygenase (COX) enzymes. Using the archazolid structure as a starting point, several simplified analogues have been prepared and assayed for their V-ATPase and COX inhibitory activity. These simplified analogues were prepared using a novel Suzuki coupling with yields over 80%. They were assayed to investigate both their V-ATPase and COX inhibitory activity. In our assays there was no COX inhibition, while there was …