Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent.

@article{Chou2010SynthesisAP,
  title={Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent.},
  author={Li-Chen Chou and Chien-ting Chen and Jang-Chang Lee and Tzong-Der Way and Chi-Hung Huang and Shih-Ming Huang and C. Teng and T. Yamori and Tian-Shung Wu and Chung-Ming Sun and D. Chien and Keduo Qian and S. Morris-Natschke and K. Lee and Li‐Jiau Huang and S. Kuo},
  journal={Journal of medicinal chemistry},
  year={2010},
  volume={53 4},
  pages={
          1616-26
        }
}
CHM-1 [2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one] (1) has a unique antitumor mechanism of action. However, because 1 has relatively low hydrophilicity, it was evaluated only via ip administration, which is not clinically acceptable. In this study, we synthesized the monosodium phosphate salt (CHM-1-P-Na, 4) of 1 as a hydrophilic prodrug. Compound 4 was rapidly converted into 1 following iv and po administration and also possessed excellent antitumor activity in a SKOV-3 xenograft nude… Expand
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