Synthesis and antitumor activities of novel dipeptide derivatives derived from dehydroabietic acid

Bioorg Med Chem Lett. 2014 Mar 15;24(6):1511-8. doi: 10.1016/j.bmcl.2014.02.001. Epub 2014 Feb 10.


A series of dipeptide derivatives from dehydroabietic acid were designed and synthesized as novel antitumor agents. The antitumor activities screening indicated that many compounds showed moderate to high levels of inhibition activities against NCI-H460, HepG2, SK-OV-3, BEL-7404, HeLa and HCT-116 cancer cell lines and that some displayed more potent inhibitory activities than commercial anticancer drug 5-fluorouracil. The mechanism of representative compound 7b was studied by AO/EB staining, Hoechst 33258 staining, JC-1 mitochondrial membrane potential staining, TUNEL assay, DNA ladder assay and flow cytometry, which exhibited that the compound could induce apoptosis in HeLa cells. Further investigation showed that compound 7b induced apoptosis of HeLa cells through a mitochondrial pathway.

Keywords: Apoptosis; Cytotoxicity; Dehydroabietic acid; Dipeptide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Abietanes / chemistry*
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Cell Line, Tumor
  • DNA Fragmentation / drug effects
  • Dipeptides / chemistry*
  • Drug Screening Assays, Antitumor
  • HCT116 Cells
  • HeLa Cells
  • Humans
  • Phenanthrenes / chemical synthesis*
  • Phenanthrenes / chemistry
  • Phenanthrenes / pharmacology*
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / chemical synthesis
  • Phenylalanine / chemistry
  • Phenylalanine / pharmacology
  • Reactive Oxygen Species / metabolism


  • Abietanes
  • Antineoplastic Agents
  • Dipeptides
  • Phenanthrenes
  • Reactive Oxygen Species
  • dehydroabietic acid
  • Phenylalanine