Structure–activity relationships of 2-, 4-, or 6-substituted estrogens as aromatase inhibitors

@article{Numazawa2005StructureactivityRO,
  title={Structure–activity relationships of 2-, 4-, or 6-substituted estrogens as aromatase inhibitors},
  author={Mitsuteru Numazawa and Momoko Ando and Yoko Watari and Takako Tominaga and Yasuko Hayata and Akiko Yoshimura},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={2005},
  volume={96},
  pages={51-58}
}
Aromatase, which is responsible for the conversion of androgens to estrogens, is a potential therapeutic target for the selective lowering of estrogen levels in patients with estrogen-dependent breast cancer. To develop a novel class of aromatase inhibitors, we tested series of 2- and 4-substituted (halogeno, methyl, formyl, methoxy, nitro, and amino) estrones (7 and 9), as well as series of 6alpha- and 6beta-substituted (alkyl, phenalkyl, and alkoxy) estrones (13 and 14), and their estradiol… Expand
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