Non-peptidic Αvβ3 Antagonists Containing Indol-1-yl Propionic Acids

K Leonard,WX Pan,B Anaclerio,JM Gushue,ZH Guo,RL DesJarlais,MA Chaikin,J Lattanze,C Crysler,CL Manthey,BE Tomczuk,JJ Marugan

Bioorganic & medicinal chemistry letters（2005）

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摘要

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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关键词

integrins,RGD mimetic,alpha(v)beta(3) antagonists

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