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

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.

• Authors: Lihui Zhao, Lina Mao, Ge Hong, Xiaojiao Yang, Tianjun Liu
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 25 Issue 12 Pg. 2540-4 (Jun 15 2015) ISSN: 1464-3405 [Electronic] England
• PMID: 25959813 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2015 Elsevier Ltd. All rights reserved.

Chemical References

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

Topics

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