Total Synthesis of Pentabromo‐ and Pentachloropseudilin, and Synthetic Analogues—Allosteric Inhibitors of Myosin ATPase

Abstract

Stopping myo: The total syntheses of the title compounds have been achieved using a highly efficient silver(I)-catalyzed cyclization of N-tosyl-homopropargylamines. The pseudilin derivatives represent a novel class of myosin inhibitors. A new allosteric binding pocket of the Dictyostelium myosin-2 motor domain has been identified for pentabromopseudilin (1) by using an X-ray crystal structure determination of the inhibitor–protein complex.