Design, synthesis and biological evaluation of novel, simplified analogues of laulimalide: modification of the side chain

Bioorg Med Chem Lett. 2005 May 2;15(9):2243-7. doi: 10.1016/j.bmcl.2005.03.018.

Abstract

Novel, simplified analogues of the microtubule-stabilizing anticancer agent laulimalide, including the first derivatives with unnatural side chains, were designed by molecular modelling, synthesized by a late-stage diversification strategy, and evaluated in vitro for growth inhibition of human ovarian carcinoma cell lines (A2780, A2780/AD10).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Cell Division / drug effects*
  • Cell Line, Tumor
  • Drug Design
  • Female
  • Humans
  • Macrolides
  • Models, Molecular
  • Molecular Conformation
  • Molecular Structure
  • Ovarian Neoplasms
  • Structure-Activity Relationship
  • Taxoids / chemical synthesis*
  • Taxoids / chemistry
  • Taxoids / pharmacology

Substances

  • Antineoplastic Agents
  • Macrolides
  • Taxoids
  • laulimalide