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.
Lihui Zhao  1 ,  Lina Mao  1 ,  Ge Hong  1 ,  Xiaojiao Yang  1 ,  Tianjun Liu  2
Affiliations
  • 1. Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin Key Laboratory of Biomedical Materials, Tianjin 300192, China.
  • 2. Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin Key Laboratory of Biomedical Materials, Tianjin 300192, China. Electronic address: [email protected].
PMID: 25959813 DOI: 10.1016/j.bmcl.2015.04.051
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.