Synthesis and biological evaluation of substituted pyrazoles as blockers of divalent metal transporter 1 (DMT1).

@article{Cadieux2012SynthesisAB,
  title={Synthesis and biological evaluation of substituted pyrazoles as blockers of divalent metal transporter 1 (DMT1).},
  author={Jay A. Cadieux and Zaihui Zhang and Maryanne Mattice and Alison Brownlie-Cutts and Jianmin Fu and Laszlo G Ratkay and Rainbow Kwan and Jay Daniel Thompson and Joseph Sanghara and Jing Xi Zhong and Yigal Paul Goldberg},
  journal={Bioorganic & medicinal chemistry letters},
  year={2012},
  volume={22 1},
  pages={90-5}
}
Three distinct series of substituted pyrazole blockers of divalent metal transporter 1 (DMT1) were elaborated from the high-throughput screening pyrazolone hit 1. Preliminary hit-to-lead efforts revealed a preference for electron-withdrawing substituents in the 4-amido-5-hydroxypyrazole series 6a-l. In turn, this preference was more pronounced in a series of 4-aryl-5-hydroxypyrazoles 8a-j. The representative analogs 6f and 12f were found to be efficacious in a rodent model of acute iron… CONTINUE READING

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