title: Synthesis and biological evaluation of novel 6-chloro-quinazolin derivatives as potential antitumor agents.
abstract: Series of novel derivatives of 6-chloro-quinazolin, which this moiety was linked to a 1,5-diaryl-1,4-pentadien-3-one system, have been synthesized and tested for their antitumor activities in vitro against a panel of three human cancer cell lines (MGC-803, Bcap-37, and PC3 cells). Bioassay results indicated that most of the prepared compounds demonstrated good activities against various cancer cells. 6-chloro-quinazolin derivatives 5a and 5f were the most active members in this study, and experimental results of fluorescent staining and flow cytometry analysis revealed that they could induce apoptosis in MGC-803 and Bcap-37 cells, with apoptosis ratios of 31.7% and 21.9% at 24 h of treatment at 10 μM in MGC-803 cells. Those two quinazoline derivatives could be considered as useful templates for future development to obtain more potent antitumor agents.
authors: Guizhou Fruit Institute, Guizhou Academy of Agricultural Sciences, Guiyang 550006, PR 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, PR China. Electronic address: luohui8732@163.com.
authors: Hui
authors: H
authors: Luo
authors: Research Institute of Traditional Chinese Medicine, Yangtze River Pharmaceutical Group Co., Ltd, Taizhou 225321, PR 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, PR China.
authors: Shengjie
authors: S
authors: Yang
authors: Guizhou Fruit Institute, Guizhou Academy of Agricultural Sciences, Guiyang 550006, PR China.
authors: Yongqiang
authors: Y
authors: Cai
authors: Guizhou Fruit Institute, Guizhou Academy of Agricultural Sciences, Guiyang 550006, PR China.
authors: Zhijun
authors: Z
authors: Peng
authors: Guizhou Fruit Institute, Guizhou Academy of Agricultural Sciences, Guiyang 550006, PR China.
authors: Tao
authors: T
authors: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D011799:Quinazolines
keywords: 6-Chloro-quinazolin derivatives; Antitumor; Apoptosis; Cancer cells; Synthesis