Design, synthesis, and preclinical evaluation of new 5,6- (or 6,7-) disubstituted-2-(fluorophenyl)quinolin-4-one derivatives as potent antitumor agents.

@article{Chou2010DesignSA,
  title={Design, synthesis, and preclinical evaluation of new 5,6- (or 6,7-) disubstituted-2-(fluorophenyl)quinolin-4-one derivatives as potent antitumor agents.},
  author={Li-Chen Chou and Meng-Tung Tsai and Mei-Hua Hsu and Sheng-Hung Wang and Tzong-Der Way and Chi-Hung Huang and Hui-Yi Lin and Keduo Qian and Yizhou Dong and Kuo Hsiung Lee and Li‐Jiau Huang and Sheng-Chu Kuo},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 22},
  pages={
          8047-58
        }
}
Our previous exploration of 2-phenylquinolin-4-ones (2-PQs) has led to an anticancer drug candidate 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na). In order to develop additional new drug candidates, novel 2-PQs were designed, synthesized, and evaluated for cytotoxic activity. Most analogues, including 1b, 2a,b, 3a,b, 4a,b, and 5a,b, exhibited significant inhibitory activity (IC(50) of 0.03-8.2 μM) against all tested tumor cell lines. As one of the most… Expand

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