Design, synthesis and anticancer activity of matrine–1H-1, 2, 3-triazole–chalcone conjugates. Issue 12 (15th June 2015)

• Record Type: Journal Article
• Authors: Zhao, Lihui; Mao, Lina; Hong, Ge; Yang, Xiaojiao; Liu, Tianjun
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 12(2015)
• Page Start: 2540
• Page End: 2544
• Publication Date: 2015-06-15
• Subjects: Matrine -- Chalcone -- 1, 2, 3-Triazole -- Conjugate -- Anticancer -- Synthesis -- Apoptosis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.04.051
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of novel matrine–1 H -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. Compounds6h and6i 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 compound6h 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.