Chalcones incorporated pyrazole ring inhibit proliferation, cell cycle progression, angiogenesis and induce apoptosis of MCF7 cell line

Anticancer Agents Med Chem. 2014;14(9):1282-92. doi: 10.2174/187152061409141010114547.

Abstract

A Series of chalcone derivatives containing pyrazole ring was prepared and their cytotoxicity against different human cell lines, including breast (MCF-7), colon (HCT-116) liver (HEPG2) cell lines, as well as normal melanocyte HFB4 was evaluated. Two of these chalcone derivatives with different IC50 and chemical configuration were chosen for molecular studies in detail with MCF-7 cells. Our data indicated that the two compounds prohibit proliferation, angiogenesis, cell cycle progression and induce apoptosis of breast cancer cells. This inhibition is mediated by up regulation of tumor suppressor p53 associated with arrest in S-G2/M of cell cycle. This work provides a confirmation of antitumor activity of the novel chalcones and assists the development of new agents for cancer treatment.

MeSH terms

  • Angiogenesis Inhibitors / chemical synthesis
  • Angiogenesis Inhibitors / chemistry
  • Angiogenesis Inhibitors / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Caspases / metabolism
  • Cell Cycle Checkpoints / drug effects*
  • Cell Proliferation / drug effects*
  • Chalcones / chemical synthesis
  • Chalcones / chemistry
  • Chalcones / pharmacology*
  • DNA Fragmentation / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • MCF-7 Cells
  • Neovascularization, Pathologic / prevention & control
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry
  • Pyrazoles / pharmacology*
  • Tumor Suppressor Protein p53 / metabolism

Substances

  • Angiogenesis Inhibitors
  • Antineoplastic Agents
  • BCL2L15 protein, human
  • Chalcones
  • Proto-Oncogene Proteins c-bcl-2
  • Pyrazoles
  • Tumor Suppressor Protein p53
  • Caspases