Novel steroid inhibitors of glucose 6-phosphate dehydrogenase.

  title={Novel steroid inhibitors of glucose 6-phosphate dehydrogenase.},
  author={Niall M. Hamilton and Martin Dawson and Emma E. Fairweather and Nicola S Hamilton and James R. Hitchin and Dominic I. James and Stuart D Jones and Allan M Jordan and Amanda J. Lyons and Helen F. Small and Graeme J. Thomson and Ian D. Waddell and Donald J. Ogilvie},
  journal={Journal of medicinal chemistry},
  volume={55 9},
Novel derivatives of the steroid DHEA 1, a known uncompetitive inhibitor of G6PD, were designed, synthesized, and tested for their ability to inhibit this dehydrogenase enzyme. Several compounds with approximately 10-fold improved potency in an enzyme assay were identified, and this improved activity translated to efficacy in a cellular assay. The SAR for steroid inhibition of G6PD has been substantially developed; the 3β-alcohol can be replaced with 3β-H-bond donors such as sulfamide… CONTINUE READING


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