Login / Signup

Design, Synthesis and Biological Evaluation of Highly Potent Simplified Archazolids.

Solenne RivièreChristin VielmuthChristiane EnnenbachAliaa AbdelrahmanCarina LemkeMichael GütschowChrista Elisabeth MüllerDirk Menche
Published in: ChemMedChem (2020)
The archazolids are potent antiproliferative compounds that have recently emerged as a novel class of promising anticancer agents. Their complex macrolide structures and scarce natural supply make the development of more readily available analogues highly important. Herein, we report the design, synthesis and biological evaluation of four simplified and partially saturated archazolid derivatives. We also reveal important structure-activity relationship data as well as insights into the pharmacophore of these complex polyketides.
Keyphrases
  • structure activity relationship
  • molecular docking
  • anti inflammatory
  • molecular dynamics
  • electronic health record
  • genome wide
  • big data
  • machine learning
  • deep learning