19-oxygenated derivatives of androst-4-ene-6,17-dione and androst-5-ene-4,17-dione as catalytic probes for the active site of aromatase.

@article{Numazawa199919oxygenatedDO,
  title={19-oxygenated derivatives of androst-4-ene-6,17-dione and androst-5-ene-4,17-dione as catalytic probes for the active site of aromatase.},
  author={M. Numazawa and K. Yamada and K. Kidokoro},
  journal={Biological & pharmaceutical bulletin},
  year={1999},
  volume={22 10},
  pages={
          1134-6
        }
}
  • M. Numazawa, K. Yamada, K. Kidokoro
  • Published 1999
  • Chemistry, Medicine
  • Biological & pharmaceutical bulletin
  • To gain insight into the binding manner of androst-4-ene-6,17-dione (4) and its 5-en-4-one analog 9, good competitive inhibitors of aromatase, in the active site of the enzyme, their 19-oxygenated derivatives were evaluated as inhibitors of human placental aromatase. The 19-hydroxy steroids 6, 7, and 10 and the 19-oxo analogs 8 and 12 were much poorer competitive inhibitors than their corresponding parent 19-methyl steroids. Conversion of the 17-keto inhibitors 4, 6, and 10 to the 17beta-ols 5… CONTINUE READING
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    Aromatase and its inhibitors in breast cancer treatment — overview and perspective
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