Non-peptidic α v β 3 antagonists containing indol-1-yl propionic acids

…, B Anaclerio, JM Gushue, Z Guo, RL DesJarlais…

Index: Leonard, Kristi; Pan, Wenxi; Anaclerio, Beth; Gushue, Joan M.; Guo, Zihong; DesJarlais, Renee L.; Chaikin, Marge A.; Lattanze, Jennifer; Crysler, Carl; Manthey, Carl L.; Tomczuk, Bruce E.; Marugan, Juan Jose Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 10 p. 2679 - 2684

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Citation Number: 26

Abstract

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.