000267865_sm_Supplement text.pdf (48.95 kB)
Supplementary Material for: Improved Synthesis of ADAM10 Inhibitor GI254023X
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posted on 2010-02-27, 00:00 authored by Hoettecke N., Ludwig A., Foro S., Schmidt B.Background: The metalloproteinases ADAM10 and ADAM17 are involved in various diseases: neurodegeneration, cancer and inflammation. Objective: The inhibition of these proteases is a promising target in the treatment of inflammation and cancer. Methods and Results: In this study, we present an improved synthesis of the ADAM10 reference inhibitor GI254023X with a higher overall yield, enhanced detection ability and increased acid stability, providing easier handling. Conclusion: This upscaled synthesis, free of diastereomeric intermediates, ensures single-batch identity, thus warranting its reproducibility in further biological investigations.