Rapamycin analogs with reduced systemic exposure

  • Bioorg Med Chem Lett. 2005 Dec 1;15(23):5340-3. doi: 10.1016/j.bmcl.2005.06.106.
Rolf Wagner  1 ,  Karl W Mollison ,  Luping Liu ,  Cynthia L Henry ,  Teresa A Rosenberg ,  Nwe Bamaung ,  Noah Tu ,  Paul E Wiedeman ,  Yatsun Or ,  Jay R Luly ,  Benjamin C Lane ,  James Trevillyan ,  Yung-Wu Chen ,  Thomas Fey ,  Gin Hsieh ,  Kennan Marsh ,  Merrill Nuss ,  Peer B Jacobson ,  Denise Wilcox ,  Richard P Carlson ,  George W Carter ,  Stevan W Djuric
Affiliations
  • 1. Abbott Laboratories, Global Pharmaceutical Research and Development, Abbott Park, IL 60064, USA. [email protected]
PMID: 16185865 DOI: 10.1016/j.bmcl.2005.06.106
Abstract

The synthesis and biological activities of rapamycin (I) analogs modified at the C-40 position are reported. Emphasis placed on compounds that potentially have an improved safety profile on account of their shorter in vivo half-life when compared with rapamycin.