title: 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.affiliation: Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin Key Laboratory of Biomedical Materials, Tianjin 300192, China.
authors.forename: Lihui
authors.initials: L
authors.lastname: Zhao
authors.affiliation: Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin Key Laboratory of Biomedical Materials, Tianjin 300192, China.
authors.forename: Lina
authors.initials: L
authors.lastname: Mao
authors.affiliation: Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin Key Laboratory of Biomedical Materials, Tianjin 300192, China.
authors.forename: Ge
authors.initials: G
authors.lastname: Hong
authors.affiliation: Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin Key Laboratory of Biomedical Materials, Tianjin 300192, China.
authors.forename: Xiaojiao
authors.initials: X
authors.lastname: Yang
authors.affiliation: Institute of Biomedical Engineering, Chinese Academy of Medical Sciences & Peking Union Medical College, Tianjin Key Laboratory of Biomedical Materials, Tianjin 300192, China. Electronic address: liutianjun@hotmail.com.
authors.forename: Tianjun
authors.initials: T
authors.lastname: Liu
mesh_terms: D000470:Alkaloids / Q000737:chemistry; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D002599:Chalcone / Q000737:chemistry*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005472:Fluorouracil / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D061986:MCF-7 Cells; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D041681:NIH 3T3 Cells; D011807:Quinolizines / Q000737:chemistry; D013329:Structure-Activity Relationship; D014183:Transplantation, Heterologous; D014230:Triazoles / Q000737:chemistry; D000093842:Matrines
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; D011807:Quinolizines; D014230:Triazoles; D002599:Chalcone; D005472:Fluorouracil; D000093842:Matrines
keywords: 1,2,3-Triazole; Anticancer; Apoptosis; Chalcone; Conjugate; Matrine; Synthesis