Improved synthesis of ADAM10 inhibitor GI254023X.

  title={Improved synthesis of ADAM10 inhibitor GI254023X.},
  author={Nicole Hoettecke and Andreas Ludwig and Sabine Foro and Boris Schmidt},
  journal={Neuro-degenerative diseases},
  volume={7 4},
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… CONTINUE READING

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