Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective αvβ3 inhibitor: Design, synthesis, and optimization

The tripeptide RGD a common binding motif in several ligands that bind to αvβ3, has been depeptidized and optimized in our efforts toward discovering a small molecule inhibitor. The cyclopropyl containing new lead compound was optimized for potency, selectivity, and for its ADME properties.