Synthesis and cytotoxicity of novel sansalvamide A derivatives

Org Lett. 2005 Aug 4;7(16):3481-4. doi: 10.1021/ol051161g.

Abstract

Described are the syntheses of 14 derivatives of the natural product Sansalvamide A, where two are more active against HCT 116 colon cancer cell lines than the natural product. These derivatives were synthesized using a combinatorial-type strategy that permits elucidation of the amino acid role in the cytotoxicity, and they lay the groundwork for development of new anticancer agents. [structure: see text]

MeSH terms

  • Antineoplastic Agents* / chemical synthesis
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Depsipeptides* / chemical synthesis
  • Depsipeptides* / chemistry
  • Depsipeptides* / pharmacology
  • Drug Screening Assays, Antitumor
  • Fusarium / chemistry*
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • Depsipeptides
  • sansalvamide A