2. Academic Validation
  3. Synthesis and biological evaluation of novel 6-chloro-quinazolin derivatives as potential antitumor agents

Synthesis and biological evaluation of novel 6-chloro-quinazolin derivatives as potential antitumor agents

  • Eur J Med Chem. 2014 Sep 12:84:746-52. doi: 10.1016/j.ejmech.2014.07.053.
Hui Luo 1,  Shengjie Yang 2,  Yongqiang Cai 3,  Zhijun Peng 3,  Tao Liu 3
Affiliations

Affiliations

  • 1 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.
  • 2 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.
  • 3 Guizhou Fruit Institute, Guizhou Academy of Agricultural Sciences, Guiyang 550006, PR China.
PMID: 25064351 DOI: 10.1016/j.ejmech.2014.07.053
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.

Keywords

6-Chloro-quinazolin derivatives; Antitumor; Apoptosis; Cancer cells; Synthesis.

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