First generation design, synthesis, and evaluation of azepine-based cryptophycin analogues

Org Lett. 2001 Dec 13;3(25):4063-6. doi: 10.1021/ol016799g.

Abstract

[structure: see text] Azepine-based cryptophycin mimics (+)-4 and (+)-5 have been designed and synthesized. Biological evaluation revealed modest in vitro activity against several human tumor cell lines, thereby supporting the utility of novel scaffolds for the design and synthesis of cryptophycin analogues.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Azepines / chemical synthesis
  • Azepines / chemistry*
  • Azepines / pharmacology
  • Crystallography, X-Ray
  • Cyanobacteria / chemistry
  • Depsipeptides
  • Drug Design*
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Peptides, Cyclic / chemical synthesis
  • Peptides, Cyclic / chemistry*
  • Peptides, Cyclic / pharmacology
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Azepines
  • Depsipeptides
  • Peptides, Cyclic
  • cryptophycin