Design, synthesis and anticancer activity of matrine-1H-1,2,3-triazole-chalcone conjugates

Bioorg Med Chem Lett. 2015 Jun 15;25(12):2540-4. doi: 10.1016/j.bmcl.2015.04.051. Epub 2015 Apr 22.

Abstract

A series of novel matrine-1H-1,2,3-triazole-chalcone conjugates was synthesized and their anticancer activity against A549, Bel-7402, Hela, and MCF-7 cancer cells was evaluated. Most of the conjugates displayed higher potency than their components. Compounds 6h and 6i exhibited more potent anticancer activity than 5-fluorouracil against the four tested human cancer cell lines and lower cytotoxicity to NIH3T3 normal cells. Flow cytometry tests demonstrated that compound 6h could induce apoptosis of A549 cells in a concentration-dependent manner. Moreover, 6h could efficiently suppress human tumor growth in mouse xenograft model without causing obvious toxicities.

Keywords: 1,2,3-Triazole; Anticancer; Apoptosis; Chalcone; Conjugate; Matrine; Synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemistry
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Chalcone / chemistry*
  • Drug Design*
  • Drug Screening Assays, Antitumor
  • Fluorouracil / pharmacology
  • HeLa Cells
  • Humans
  • MCF-7 Cells
  • Male
  • Matrines
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • NIH 3T3 Cells
  • Quinolizines / chemistry
  • Structure-Activity Relationship
  • Transplantation, Heterologous
  • Triazoles / chemistry

Substances

  • Alkaloids
  • Antineoplastic Agents
  • Quinolizines
  • Triazoles
  • Chalcone
  • Fluorouracil
  • Matrines