Non-peptidic αvβ3 antagonists containing indol-1-yl propionic acids

We describe the synthesis and structure/activity relationship of RGD mimetics that are potent inhibitors of the integrin αvβ3. Indol-1-yl propionic acids containing a variety of basic moieties at the 5-position, as well as substitutions alpha and beta to the carboxy terminus were synthesized and evaluated. Novel compounds with improved potency have been identified.

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