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Design, synthesis, and biological activities of madindoline analogues. | LitMetric

Design, synthesis, and biological activities of madindoline analogues.

Bioorg Med Chem Lett

The Kitasato Institute, and Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, School of Pharmaceutical Sciences, Kitasato University, Japan.

Published: May 2006

AI Article Synopsis

  • * Madindoline is not available from natural sources, so a synthetic method has been developed to produce it.
  • * Tests on various madindoline analogues revealed several strong candidates for fighting IL-6-dependent diseases.

Article Abstract

A research program is under way to develop a series of madindoline-based inhibitors targeting interleukin 6. Such inhibitors will have potential use in fighting a variety of diseases for which no effective therapeutic drugs currently exist. Madindoline is no longer available from natural sources. Consequently, we have developed a purely synthetic route to ensure a supply of the compound. The synthesis of a range of analogues is described, all of which were evaluated for their inhibitory activity against the growth of IL-6-dependent 7TDI cells. From these assays, several synthetic madindoline analogues were identified as highly promising candidates for further development.

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Source
http://dx.doi.org/10.1016/j.bmcl.2006.01.107DOI Listing

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