title: Synthesis and in vitro antitumor activity of (1E,4E)-1-aryl-5-(2-((quinazolin-4-yl)oxy)phenyl)-1,4-pentadien-3-one derivatives.
abstract: BACKGROUND
  Cancer is one of the leading causes of death and only second to heart diseases. Recently, preclinical studies have demonstrated that curcumin had a number of anticancer properties. Thus, we planned to synthesize a series of curcumin analogs to assess their antiproliferation efficacy.
  
  
  RESULTS
  A series of (1E,4E)-1-aryl-5-(2-((quinazolin-4-yl)oxy)phenyl)-1,4-pentadien-3-one derivatives (curcumin analogs) were synthesized and characterized by IR, NMR, and elemental analysis techniques. All of the prepared compounds were screened for antitumor activities against MGC-803, PC3, and Bcap-37 cancer cell lines. A significant inhibition for cancer cells were observed with compound5fand also less toxic on NIH3T3 normal cells. The mechanism of cell death induced by compound5fwas further investigated by acridine orange/ethidium bromide staining, Hoechst 33,258 staining, TUNEL assay, and flow cytometry cytometry, which revealed that the compound can induce cell apoptosis in MGC-803 cells.
  
  
  CONCLUSIONS
  This study suggests that most of the derivatives could inhibit the growth of human cancer cell lines. In addition, compound5fcould induce apoptosis of cancer cells, and it should be subjected to further investigation as a potential anticancer drug candidate.
authors.affiliation: Guizhou Fruit Institute, Guizhou Academy of Agricultural Sciences, Guiyang, 550006 P. R. China.|State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, 550025 P. R. China.|Ctr for R&D of Fine Chemicals, Guizhou University, Guiyang, 550025 P. R. China.
authors.forename: Hui
authors.initials: H
authors.lastname: Luo
authors.affiliation: R&D Center, Sinphar Tian-Li Pharmaceutical Co., Ltd, Hangzhou, 311100 P. R. China.|State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, 550025 P. R. China.|Ctr for R&D of Fine Chemicals, Guizhou University, Guiyang, 550025 P. R. China.
authors.forename: Shengjie
authors.initials: S
authors.lastname: Yang
authors.affiliation: R&D Center, Sinphar Tian-Li Pharmaceutical Co., Ltd, Hangzhou, 311100 P. R. China.
authors.forename: Da
authors.initials: D
authors.lastname: Hong
authors.affiliation: State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, 550025 P. R. China.|Ctr for R&D of Fine Chemicals, Guizhou University, Guiyang, 550025 P. R. China.
authors.forename: Wei
authors.initials: W
authors.lastname: Xue
authors.affiliation: Guizhou Fruit Institute, Guizhou Academy of Agricultural Sciences, Guiyang, 550006 P. R. China.
authors.forename: Pu
authors.initials: P
authors.lastname: Xie
keywords: Antitumor activity; Apoptosis; Asymmetric curcumin analogs; MGC-803; Quinazoline derivatives of curcumin; Synthesis