Design and synthesis of selective inhibitors of Placental Alkaline Phosphatase

Placental Alkaline Phosphatase (PLAP) is a tissue-restricted isozyme of the Alkaline Phosphatase (AP) superfamily. PLAP is an oncodevelopmental enzyme expressed during pregnancy and in a variety of human cancers, but its biological function remains unknown. We report here a series of catechol compounds with great affinity for the PLAP isozyme and significant selectivity over other members of the AP superfamily. These selective PLAP inhibitors will provide small molecule probes for the study of the pathophysiological role of PLAP.

A series of catechols was selected and evaluated as selective inhibitors of PLAP over the other AP isozymes. SAR is reported.Figure optionsDownload as PowerPoint slide